Day 17 :
- Medicinal Chemistry | Natural Chemistry
Chair
Cornelia G Palivan
University of Basel, Switzerland
Co-Chair
Laura B Sagle
University of Cincinnati, USA
Session Introduction
Aiichiro Nagaki
Kyoto University, Japan
Title: Synthesis of organofluorine compounds using flow microreactors
Time : 11:45-12:15
Biography:
Aiichiro Nagaki received his PhD from Kyoto University under the supervision of Professor Jun-ichi Yoshida in the year 2005. He worked with Professor Hiroaki Suga, Tokyo University in 2005 as a Post-doctoral Fellow. In 2006, he became an Assistant Professor of Kyoto University. He was promoted to Junior Associate Professor in the year 2013. His current research interests are organic synthesis, polymer synthesis, and microreactor synthesis. He has won many awards: Takeda Pharmaceutical Co., Ltd. Award in Synthetic Organic Chemistry, Japan (2012); Incentive Award in Synthetic Organic Chemistry, Japan (2012) and; Young Innovator Award on Chemistry and Micro-Nano Systems (2013).
Abstract:
Organo-fluorine compounds are the substances of considerable interest in various industrial fields due to their unique physical and chemical properties. Despite increased demand in wide fields of science, synthesis of organofluorine compounds is still often faced with problems. Recently, flow microreactor synthesis has emerged as a new methodology for producing chemical substances with high efficiency. Here, we report a flow microreactor method for the synthesis of organofluorine compounds based on the generation of unstable fluoro- substituted organolithiums involving perfluoroalkyllithiums and subsequent reactions that are not compatible with the generation process.
John H. Summerfield
Missouri Southern State University, USA
Title: A Drug Delivery Model: 5-fluorouracil Intercalated into Montmorillonite Investigated to the Hartree-Fock Level
Time : 12:15-12:45
Biography:
Education: Ph.D, Oregon State University (Physical Chemistry), 1994 Teaching Responsibilities: Physics for non-science students, General Chemistry, Physical Chemistry, Organic Chemistry lab Specialties/Research Interests: Computer models of lithium ion batteries. Computer models of clays as a drug delivery method Advising Areas: Chemistry, Biochemistry, Medical Technology Personal Interests: Canoeing, Traveling to Central America, Gardening
Abstract:
Molecular mechanics calculations, based on equations such as the one below, are used to investigate a colorectal cancer drug, 5-fluorouracil, intercalated into a clay, montmorillonite. This combination is currently being considered as a drug delivery system. The swelling of clays has been studied since the 1930s and is still not fully understood. Spartan ’14 is used for the calculations. Semi-empirical and ab initio basis set scaling is also examined since there are roughly 300 atoms involved in the full model.
Sulaiman Al-Zuhair
UAE University, UAE
Title: Regeneration of amine solution using microalgae for absorption
Time : 12:45-13:15
Biography:
Sulaiman Al-Zuhair is a Professor and Coordinator of the MSc Program in the Chemical Engineering Department at UAE University. He earned a PhD in Biochemical Engineering from the University of Malaya (2003). Before joining UAE University, he held the position of Assistant Professor at the University of Nottingham, Malaysia campus. He published 1 book, 54 journal papers, 2 patents and 2 book chapters. Majority of his research work is on the uses of enzymes in various industrial applications. He has been serving as an Editorial Board Member of several reputable journals
Abstract:
The removal of CO2 for natural gas sweetening or flue gas treatments is most commonly done through absorption using aqueous amine solutions, due to their high capturing efficiency. However, the high energy demand of the stripping step, conventionally used to regenerate the solvents, after the absorption process is completed, remains the main challenge facing the overall absorption process. The high energy requirements in the regeneration raises the energy penalty of CO2 capture by amine solvents in a fossil fuel power plant to about 23–30% of the energy output. In this work, the ability of microalgae to regenerate amine solutions saturated with CO2 has been tested, with a far lower energy requirements. In addition, the harvested microalgae can be readily used to produce valuable products, such as lipids, proteins, and pigments. Two strains of microalgae (Chlorella sp. and Pseudochlorococcum sp.) and two amine solutions (10% DEA and 10% MEA) were investigated at different light intensities. The microalgae growth rate and the drop in dissolved CO2 concentrations were monitored. Both strained behaved better in MEA solution, compared to DEA. With faster regeneration achieved using Pseudochlorococcum sp. The increased light intensity had a negative effect on the performance.
Laura B Sagle
Researcher, USA
Title: Current Challenges And Approaches For Improved Localized Surface Plasmon Resonance Biosensing
Time : 14:00-14:30
Biography:
Laura Sagle has completed her PhD in 2006 from University of California San Diego under the direction of Prof. Floyd Romesberg at the Scripps Research Institute. She then carried out postdoctoral research in the laboratory of Prof. Paul Cremer followed by another postdoc in the lab of Prof. Richard Van Duyne. The Sagle group currently carries out research at the biology-nanoscience interface, focused on improved LSPR biosensing and single molecule biophysical surface enhanced Raman spectroscopy.
Abstract:
Biosensing utilizing Localized Surface Plasmon Resonance (LSPR) offers relatively inexpensive, label-free, facile detection that is amenable to on-chip devices. Such devices can provide exquisite sensitivity at a low cost and should prove extremely useful in resource limited environments. However, several challenges remain, such as: sensitivity to small molecule binding, specificity in complex biological solutions, detection of membrane-associated species and integration into on-chip devices. This presentation will highlight recent advances in LSPR-based biosensing devices developed in the Sagle group to overcome these limitations. One study we have done to increase sensitivity is an assay in which gold nanostars are aggregated upon addition of an analyte. Due to increased surface area of contact, a large decrease in Kd and limit of detection in the attomolar range was observed with this simple aggregation assay. In addressing the second challenge, we have incorporated shape complementarity on the nanoparticle surface to carry out size-selective biosensing with improved selectivity. The third challenge is tackled through the development of a novel plasmonic platform containing a solid supported lipid bilayer so that label-free measurements of membrane associated species can be carried out. This device is shown to have improved sensitivity over existing platforms. Lastly, large-scale patterning of the nanoparticle arrays enabling the interfacing of these arrays with microfluidic, on-chip devices are also presented.
Cornelia G Palivan
University of Basel, Switzerland
Title: Artificial organelles: How nanoscience provides therapeutic solutions
Time : 14:30-15:00
Biography:
Cornelia G. Palivan is Professor in Physical Chemistry at the University of Basel, Switzerland. She received several awards for her research, and published more than 100 publications. Her interest is on development of hybrid materials (nanoreactors, active surfaces, artificial organelles, nanodevices, functional membranes) by combining biomolecules or mimics with synthetic supramolecular assemblies for medical, environmental, technological, and food science oriented applications.
Abstract:
Because organelles are key components in cells and comprise compartments loaded with molecules essential to life, their inadequate functioning can contribute to numerous pathological conditions. Creating artificial organelles that aid their natural counterparts in cells will have a dramatic impact on medicine in the treatment of disorders and in the design of artificial cells. To design artificial organelles, nanoscience provides a necessary tool, the self-assembly of amphiphilic copolymers into supramolecular structures such as micelles, tubes, and vesicles. They represent ideal candidates to form organelle-like compartments that can contain combinations of biomolecules. Here, we show the necessary steps for the development of an artificial organelle able to act in situ inside cells. The artificial organelle is based on two enzymes in tandem encapsulated in polymer vesicles with membrane rendered permeable by inserted channel proteins. Polymer vesicles play a dual role: they protect the enzymes from proteolytic attack and allow them to act inside their cavity. An example of the first artificial peroxisome is presented as model for nanosciance based strategy to design artificial organelles. Uptake, absence of toxicity, and in situ activity in cells exposed to oxidative stress demonstrated that the artificial peroxisomes detoxify superoxide radicals and H2O2 after endosomal escape. Our artificial peroxisome combats oxidative stress in cells, a factor in various pathologies (e.g. arthritis, Parkinson’s, cancer, AIDS), and offers a versatile strategy to develop other “cell implants” for cell dysfunction.
Anupreet Kaur
Punjab University, India
Title: Synthesis, Characterisation and biotransformation of novel 1,4-dihydropyridine derivatives
Time : 15:00-15:30
Biography:
Anupreet Kaur is serving as an Assistant Professor at UIET, Panjab University Chandigarh, India. She has completed her Master’s in Chemical Engineering and is pursuing her PhD in Biotechnology.
Abstract:
Chiral molecules are the molecules which possess non-superimposable mirror image, referred as enantiomers. Stereoisomerism may result in altogether varied pharmacological activity and potency. In this regard, a drug molecule with a single chirality would render to be more selective with improved therapeutic benefits compared to racemic analogues. Such stereoisomerism necessitates the thorough assessment of pharmacological and toxicological studies. Separation of such enantiomers has been possible with the emergence of new technologies in the last few decades before which majority of the drugs were marketed as racemates.1, 4-dihydropyridine is a calcium channel blocker generally used in the treatment of hypertension. Novel analogues of this class have been synthesized in our lab via microwave irradiation. Microwave heating is considered to be a green approach as it makes use of the solvent which is rapid and eco-friendly. The structures for the same compounds were confirmed with the help of NMR, IR and MS analysis. The synthesized compounds were subjected to enzymatic hydrolysis using majorly Candida antarctica, Pseudomonas lipases anticipating the induction of chirality. The results for the same have been established using chromatography methods which have been optimised for these compounds in terms of mobile phase composition, temperature, types of columns and flow rate so as to characterise these compounds in the shortest time. The retention time for all these compounds has been optimised to be less than 10 minutes. Their standard curves have been found to be linear over the concentration range of 10-60 µg ml-1. It has been demonstrated that the validated methods are simple, rapid, specific and reproducible and hence can be of great utility in the routine analysis of these drugs.
Adit Sharan
Micro Labs Ltd., India
Title: Anti-inflammatory and antinociceptive activity of vanillin
Time : 15:30-16:00
Biography:
Adit Sharan has done Bachelor in Pharmaceutical Sciences from Rayat-Bahra Institute of Pharmacy, Hoshiarpur with affiliation to Punjab Technical University (Jalandhar). Currently he is working for Micro Labs Ltd., since November 2012. He is a member of FIP (International Pharmaceutical Federation), The Hague, The Netherlands.
Abstract:
Objective: Vanillin is known to have antimutagenic, anti-invasive, and metastatic suppression potential. Antinociceptive property in acetic acid and antioxidant and hepatoprotective properties in carbon tetrachloride treated rats have also been demonstrated. Objective of this study is to evaluate the anti-inflammatory and antinociceptive activity of vanillin.
Materials and Methods: The drugs and fine chemicals were purchased from Sigma Aldrich, Ranbaxy, India and MS Pharmaceuticals, India. Experimental Rats were assigned to groups of six animals each and anti-inflammatory activity was evaluated using carrageenan induced rat paw aedema and anti-nocicetion was done using tail flick method. Carrageenan induced paw edema was used to evaluate pre and post anti-inflammatory activity and tail flick method was used in the evaluation of antinociceptive activity. Two-way analysis of variance (ANOVA) followed by Student’s t-test was used for statistical analysis in both the studies.
Results: There was significant decrease in the paw volume at 50 and 100mg/kg doses of vanillin when compared with control group. Meanwhile, an increase in percentage maximum possible effect (MPE) was seen by same doses of vanillin.
Conclusion: It has been concluded from the findings that vanillin possesses the anti-inflammatory and antinociceptive effect by virtue of its anti-histaminic and central analgesic activity, respectively.
Alireza Doroudi
Ahvaz Jundishapur University of Medical Sciences, Iran
Title: The application of ultrasound irradiation technique for the reconstitution of radiopharmaceutical kits
Time : 16:00- 16:30
Biography:
Alireza Doroudi has completed his PhD in 2005 from Tehran University of Medical Sciences. He is a Radiopharmacist, Associated Professor and Director of research team focusing on new developed technique for reconstitution kits, preparation of new radiotracer for diagnosis of infection and bone pain palliation therapy and synthesis of new radiosensitizer compounds. He has published more than 20 papers in reputed journals.
Abstract:
Sonochemistry is a branch of chemical research dealing with the application of ultrasound waves. Green chemistry has successfully improved the yield of the reactions, changed the reaction pathway or initiated the reaction. Technetium 99m 2-methoxy isobutyl isonitrile is a lipophilic cation complex that has been accumulated in viable myocardial tissue by passive diffusion into myocyte with subsequent binding to the mitochondria within the cell. This radiotracer has been demonstrated suitable characteristics for myocardial perfusion studies. The freeze dried kit of sestamibi contains 2-methoxy isobutyl isonitirle (Sestamibi) as a performed copper (I) complex, which facilitates labeling by ligand exchange at elevated temperature. The labeling process of MIBI as a conventional method is time-consuming. It is highly desirable to reduce the time of labeling process particularly in emergency situations in clinical practice. In our previous study, 37 MBq(1mCi) 99mTc-MIBI samples with appropriate yields could be reconstituted under ultrasound irradiation technique. Then the activity was scaled up to the amounts that could be used for myocardial perfusion imaging. The new developed technique has been suggested for preparation of 99mTc-MIBI in clinical practice. We continued our achievement to the other radiopharmaceutical kit which the reconstitution is time-consuming in nuclear medicine departments.
Mitchell S. Albert
Lakehead University, Canada
Title: Advances in MRI Using Hyperpolarized and Inert Gases and Molecular MR Imaging
Biography:
Dr. Albert is a Research Chair at the Thunder Bay Regional Research Institute and Lakehead University. He is Director of MRI Research, Director of the Hyperpolarized Gas MRI Laboratory, a Scientist at TBRRI, and Professor of Chemistry at Lakehead University. Prior to this he was Associate Professor of Radiology at the Harvard Medical School. Dr. Albert is one of the inventors and pioneers of hyperpolarized gas MRI, and holds 9 patents on its development. He received the United States Presidential Award from President Clinton for this invention and received a CAREER award from the National Science Foundation (NSF).
Abstract:
Hyperpolarized (HP) agents have the potential to vastly improve MRI sensitivity for the diagnosis and management of various diseases. The polarization of 3He and 129Xe can be enhanced by a factor of up to 100,000, which enables direct detection of the HP agent with no background signal. Conventional 1H MR imaging of the lungs is very challenging, particularly due to the low proton density in lung tissue. HP gas MRI, using 3He or 129Xe, can be used to obtain high-quality images of the lung structure and function. Inert fluorinated gas 19F MRI is a new pulmonary imaging modality that may be able to provide images and functional information similar to HP gas MRI. Inert fluorinated gases are nontoxic, abundant, inexpensive, and do not need to be hyperpolarized prior to their use in MRI, and their short T1 allows for signal averaging within a breath-hold. HP 129Xe is a potentially valuable MR tracer for functional brain imaging due to its high solubility in the blood and brain, and its large chemical shift range. We published the first results using HP 129Xe brain imaging techniques for the measurement of cerebral ischemia and cortical brain function in rats. HP 129Xe can also be used in biosensors for molecular MR imaging, and delivered to a target by means of dedicated molecular cage systems that can encapsulate xenon and bind to biological sites of interest using a targeting moiety, such as an antibody or a ligand, which enables detection of a specific biomarker.
Thirumeni Subramanian
Saiva Bhanu Kshatriya College, India
Title: Cu(I)-Y Zeolite catalyzed Amination of Aryl Halides and Arylboronic Acids with Aqueous Ammonia
Biography:
Myself Dr. T. Subramanian completed my Ph.D., at the age of 29 years from Madurai Kamaraj University, India. I have been awarded of Post-Doctoral Fellow from University of South Dakota, SD, USA. Got award of UGC-JRF & SRF from Government of India. Now I am working as a assistant professor in Department of Chemistry, Saiva Bhanu Kshatriya College, Aruppukottai, Tamil Nadu, India. I have published more than 10 papers in reputed journals. Attended more than 10 International and 20 National Conference. I have visited two countries such as USA and France.
Abstract:
A simple, green, clean and reusable method is developed for the synthesis of primary aromatic amines from aryl halides and arylboronic acids using aqueous ammonia and Cu(I)-Y zeolite as a heterogeneous catalyst. Using this very convenient, inexpensive, reusable and practical approach, a variety of substituted aryl halides and arylboronic acids are readily aminated. Amination processes ï¬nd applications in the production of aminopyridines and pyrroles. Use of these homogeneous catalysts are generally connected with problems in separation, recovery and regeneration of the catalysts which can be minimised using a heterogeneously catalyzed reaction. Zeolites/clays are capable of stabilising small metal particles and can maintain their activity. In addition, zeolites are known for their shape selectivity, which can enhance the selectivity of the heterogeneous catalysis. This procedure outlined here is highly competitive with existing copper based catalysts and it can be readily adopted in custom synthesis and industrial processes. This coupling reaction involving ammonia was performed under nitrogen atmosphere at room temperature without the need for sealed reaction set-up, no external ligand to stabilize the metal ion, easy separation and avoids unwanted side reactions. This efficient copper catalyzed method is also successfully studied for the synthesis of primary aromatic amines by coupling of arylboronic acids. It is relevant to note here that in a recent review on catalytic organometallic reactions of ammonia, Hartwig has highlighted a few remaining goals to be accomplished in this vital area. The present work fulfils two of these challenges, namely lower temperature and reaction of ortho-substituted aryl halides. Further studies are underway to expand the scope of this method to other related synthetic applications.
- Natural Chemistry
Session Introduction
Tulio Chavez-Gil
Coppin State University, USA
Title: Bio-Inorganic non-ï¢-lactamase Metallo-Antibiotics
Biography:
Dr. Tulio Chavez-Gil is currently an Assistant Professor of Chemistry at Coppin State University, Baltimore, MD. He got his BS in Chemistry at Universidad del Valle (Cali, Colombia) where he worked as Researcher Assistant designing the Coals and Petroleum Lab in the School of Engineering. He earned his PhD in Inorganic Chemistry at Universidade de São Paulo, (São Paulo, BR) in 1997. He spent two years (1997-1999) as postdoctoral fellow at University of Kumamoto (Japan) and other two (2000-2002) at University of Puerto Rico - Mayaguez. His academic accomplishments include positions at Universidad de Los Andes (Bogota, Col - 2003), Inter-American University of Puerto Rico (2004-2014). Dr. Chavez-Gil has authored/coauthored 27 peer-reviewed publications (five in geology), one patent application and more than 70 research/educational presentations. He has been awarded with the Cnpq scholarship award (BR), the Japan Society for the Promotion of Science (JSPS), the MBRS-NIH award (UPR), and the Ronald E McNair mentorship award 2007-2014 at IAUPR. He is an editorial board member in the Structural Chemistry & Crystallography Communication Journal.
Abstract:
The fast emerging in antimicrobial resistance has been the timely challenge for all classes of antibiotics, temporarily assuaging the concerns of modern medicine. Nowadays, there has been a significant retraction on the drugs design and research investment to attain new antimicrobial medicines by the major pharmaceutical companies with the coinciding escalation in global nosocomial infection. Metallo-antibiotic compounds has been less related with medicine applications and here we are presenting new results about the antimicrobial activity of a series of chelators having N and O functionalities and its vanadium complexes as a lane of research developed with particular emphasis to test its antibiotic activity against the emergent so called “ESKAPE†super bugs. Some of the most serious infection caused by ESKAPE strains is bateremia, pneumonia, osteomyelitis, acute endocarditis, myocarditis, pericarditis, cerebritis, meningitis, chorioamnionitis, scalded skin syndrome, abscesses of the muscle, urogenital tract, central nervous system, and various intra abdominal organs. The proposed artificial antibiotics and its derived complexes has being synthesized between dipicolonic acid (found in bacteria’s cell wall), 2-methylsalycilate, anthranilic acid, and NH4VO3. Those nonï€ï¢ï€lactamase chelators and its vanadium compounds, still acting as either cytotoxic or bacteriostatic agents against a broad scope of bacteria strains. The in vitro preliminary screening with Gram-(positive/negative) strains suggests powerful growth inhibition activity on different bacteria viz., Staphylococcus aureus; Staphylococcus epidermidis; Bacillus cereus; Streptococcus faecalis; Acinetobacter bawmannii; Citrobacter freundii; Salmonella typhimurium; Serratia marcenses; Escherichia coli; Enterobacter aerogenes; Enterobacter cloacae; Klebsiella pneumoniae; Pseudomonas aeruginosa, and Proteus vulgaris.
Aiichiro Nagaki
Kyoto University, Japan
Title: Synthesis of Organofluorine Compounds Using Flow Microreactors
Biography:
I received his Ph.D. in 2005 from Kyoto University under the supervision of Professor Jun-ichi Yoshida. I worked with Professor Hiroaki Suga, Tokyo University from 2005 as a postdoctoral fellow. In 2006, he became an assistant professor of Kyoto University. I was promoted to junior associate professor in 2013. My current research interests are organic synthesis, polymer synthesis, and microreactor synthesis. Awards: Takeda Pharmaceutical Co., Ltd. Award in Synthetic Organic Chemistry, Japan (2012), Incentive Award in Synthetic Organic Chemistry, Japan (2012), and Young Innovator Award on Chemistry and Micro-Nano Systems (2013).
Abstract:
Organo-fluorine compounds are the substances of considerable interest in various industrial fields due to their unique physical and chemical properties. Despite increased demand in wide fields of science, synthesis of organofluorine compounds is still often faced with problems. Recently, flow microreactor synthesis has emerged as a new methodology for producing chemical substances with high efficiency. Here we report a flow microreactor method for the synthesis of organofluorine compounds based on the generation of unstable fluoro- substituted organolithiums involving perfluoroalkyllithiums and subsequent reactions that are not compatible with the generation process.
Biography:
Kasmiati is Ph.D candidate at Nagoya University Graduate Shcool of Bioagricultural Sciences, field of bioactive natural products chemistry. She is a young lecturer at Hasanuddin University Indonesia Faculty of Marine Sciences and Fishery. She has presented related papers both poster and oral in some international conferences.
Abstract:
Marine natural products have been providing structurally novel bioactive substances, some of which were developed as medicines or were promising leads for new drugs. During the search for bioactive substances from marine organisms, we detected anti-phytophatogenic (an oomycete of Phytophthora) activity for extracts of the Indonesian red seaweed Laurencia intricata. The active hexane and 90% methanol extracts were combined and separated on silica gel and then purified by reversed-phase HPLC to obtain four related compounds. Based on 2D NMR and MS analysis, they were identified as aplysistatin, palisadin A, palisol, and 5ï¢-hydroxypalisadin B, which are all known brominated sesquiterpenes. The minimum doses to inhibit Phytophthora capsici are 100, 300, 300, and 300 ïg/disk, respectively. Cytotoxic activity of these compounds was also evaluated against human epidermoid carcinoma A431 cells, showing the IC50 values of 0.15, 1.42, 0.59, and 0.45 ïg/ml, respectively.
Ayesha Fatima
Pharmacist, Malaysia
Title: Zerumbone modulation of the beta-catenin-TCF4 binding to induce apoptosis in cancer cells
Biography:
I, Ayesha Fatima, am a pharmacist with more than 10 years of academic experience. My research experience is spanned over the last 5 years during which I am also persuing my PhD on anti-cancer drugs and signalling pathways. My research interests have focused on computational investigations of drug-protein binding and the information that can be elucidated about the mechanisms of protein inhibition.
Abstract:
The Wnt-beta catenin pathway has been explored in several cancers. Aberration in the beta catenin inhibitory complex is thought to be the major cause for its uninhibited nuclear translocation and proliferation of cancer cells. Zerumbone, a sesquiterpene from Zingiber zerumbet Smith., has shown an excellent effectiveness as anticancer by inducing apoptosis in a time-dependent and concentration-dependent manner. Using computational techniques, this study aimed to predict the targets of Zerumbone in the pathway and to understand their binding mechanism. Our results showed that beta catenin-TCF4 complex could be the targets of Zerumbone. The binding free energy of beta catenin-TCF4 complexes from docking and molecular mechanics are -80 kcal/mol and -11. 9 kcal/mol, respectively. QM/MM method was used to estimate the effect of binding dynamics in the critical binding area between beta catenin-TCF4. It was found that the binding free energy was -29 kcal/mol in the QM region. From the results of steered molecular dynamics, the force required to pull the TCF4 peptide from the beta catenin in the presence of Zerumbone was almost similar, however it took slightly longer time to pull the chain. Wet laboratory results also confirmed that Zerumbone inhibits beta catenin nuclear translocation in HEPG2 cell line, however same results were not observed for MCF7. Hence, Zerumbone can strongly modulate the binding of beta catenin with TCF4 in a time-dependent manner thus altering the cellular pool of cell proliferating proteins. Further analysis still requires to unveil the mechanisms of the inhibition process of beta catenin and TCF4-DNA complex.
- Clinical Chemistry
Session Introduction
Hany F. Sobhi
Coppin State University, USA
Title: Synthesis & spectroscopic characterization of acyl carnitine derivatives, for the diagnosis of fatty acid β-oxidation disorder
Biography:
Dr. Sobhi obtained his Ph.D. in Clinical Bioanalytical Chemistry, from Cleveland State University in 2008, following his M.S. in Synthetic organic Chemistry in 2005. In 2008 he was appointed as NIH Post-Doctoral Fellow, at Case Western Reserve University, School of Medicine. Dr. Sobhi is an Associate Professor, and director of Coppin center for organic synthesis at Coppin State University. He is an active researcher in translational research that focused on the development strategies to synthesis small bioorganic molecules for clinical diagnosis. Dr. Sobhi received several awards from AACR, NASA and most recently the 2015 Wilson L. Elkins Professor of Chemistry
Abstract:
β-Oxidation of acyl-CoAs in mitochondria [1] produces various acylcarnitines that appear in blood and are excreted into urine. Acylcarnitine profiles have been used as biomarker for the diagnoses specific inherited metabolic diseases, [2] such as medium-chain acyl- CoAdehydrogenase deficiency (MCAD) [3], (MADD) [4], (VLCAD) [5], and long-chain hydroxyacyl-CoA dehydrogenase deficiency (LCHAD) [6] by using tandem mass spectrometry. Carnitine acyltransferace enzymes reversibly interconvert acyl-CoA and, acylcarnitine derivatives, thereby it catalyze the translocation of the fatty acyl moiety across the mitochondrial membrane. The identification of the carnitine ester has not been recognized by tandem mass spectrometry. We have established a method based on O-Acylation of carnitine chloride, and /or replacement of the acid chloride by equimolecular amount of thionyl chloride followed by the addition of carnitine chloride. We have synthesized of a series of Acyl-carnitine derivatives such as Cis-5- , and Trans-5 Tetradecenoyl carnitine carnitine, and Trans -2-Tetradecenoyl carnitine. The synthesized carnitine derivatives was fully characterized by NMR, GC/EI-MS, LC/MS. The isolation of the C14:1 acylcarnitine from human urine, will be transesterified to form ester derivative, and characterized, these results will be compared to those standard carnitines. The standards will then spiked in urine, and detected by HPLC/MS. Based on the data that we expect from the analyses we can develop an assay for the detection of the acyl carnitine. Following the same methodology we will synthesis several Acyl carnitine derivatives and develop a general Chromatography based assay for detection of small , Medium a, and long chains Acyl carnitine in urine.
- Inorganic Chemistry | Nuclear Chemistry
Chair
Sulaiman Al-Zuhair
UAE University, UAE
Session Introduction
Naghi Saadatjou
Semnan University, Iran
Title: The effect of hydrogen and chemical treatments of activated carbon in the synthesis of Ammonia on the promoted Ruthenium catalyst
Time : 10:00- 10:30
Biography:
Naghi Saadatjou has completed his PhD from University of Leeds (UK) and worked in Petro-Canada Lubricants R&D, Mississauga, Canada as a Research Chemist. He is now Senior Researcher, Professor of Applied Chemistry and Director of a research team focusing on Petrochemicals and Polymers at Semnan University and Petrochemical Research and Technology Company, Iran. He has published more than 50 papers in reputed journals and serving as an Editorial Board Member of some related journals.
Abstract:
In this work, the activated carbon without any treatment (AC), AC with hydrogen treatment at 900 °C for 24 h (ACH) and ACH with HNO3 treatment at 90 °C for 5h in the reflux system (ACHN) were used as a support for ruthenium catalyst. They were impregnated by RuCl3, Ba(NO3)2 and KOH solutions, then were reduced by H2 at 400°C for 4 h. They were used as ammonia synthesis catalyst. The physical and chemical properties of catalyst samples were characterized by applying nitrogen adsorption/desorption, TEM, SEM, EDS and XRD methods. The ammonia synthesis activity was evaluated in the fixed-bed reactor set-up under near-commercial operating conditions (that is, T: 400-450°C, P: 30 bar, H2/N2:3/1). It was found that the treatment of activated carbon support with hydrogen (ACH) and hydrogen/HNO3 (ACHN) significantly enhanced both activity and stability of catalysts although the textural properties little influenced. According to the support type, the order for both activity and stability was ACHN>ACH>AC. The best performance was obtained for K-Ba-Ru/ACHN sample due to the removal of chlorine and sulfur impurities and formation of oxygen-containing surface functional groups after hydrogen and HNO3 treatment of AC support that resulted to good dispersion of Ru and promoters. The reaction was found not to be intra-particle diffusion limited. A second order rate expression was proposed for deactivation kinetics of the catalysts and numerical values of 0.016 and 0.0018 h-1 were obtained for rate constant of deactivation of K-Ba-Ru/ACH and K-Ba-Ru/AC catalysts, respectively.
Shashi Bala Kalia
Himachal Pradesh University, India
Title: Catalytic, biological activity and thermal behaviour of triphenylphosphine capped zinc sulfide nanoparticles
Time : 10:30-11:00
Biography:
Shashi Bala Kalia has completed her PhD from Punjabi University, Patiala and worked as Post-doctoral Fellow at Himachal Pradesh University, Shimla. She is Chairperson of Chemistry at Department of Himachal Pradesh University, Shimla. She has published more than 60 papers in reputed journals of national and international repute.
Abstract:
Synthesis of ZnS nanoparticles in toluene solution using triphenylphosphine as capping agent has been carried out. EDAX analysis confirmed the composition of zinc sulfide nanoparticles. Field Emission Scanning Electron Microscope images revealed that zinc sulfide nanoparticles are of spherical shape. TEM study showed spherical mono dispersed particles ranging in size 13-19 nm. XRD spectrum peaks corresponding to (111) and (220) show that the zinc sulfide nanoparticles are crystalline in nature having zinc blende structure. FTIR spectroscopy shows the presence of triphenylphosphine as capping agent. Surface plasmon resonance peak at 293 nm in the UV spectrum indicates presence of zinc sulfide nanoparticles which correspond to band gap of 4.23 eV. Room temperature photoluminescence spectrum of the powder showed three peaks centred on 325 nm (3.81 eV), 397 nm (3.12 eV) and 425 nm (2.91 eV). Thermal behaviour of nanoparticles exhibited single step decomposition (84%) between 250oC to 350oC and ZnS as final residual product (16%). Degradation efficiency of the nanoparticles for dyes methyl orange, congo red and rodamine G6 after 3 h irradiation time was more than 90% thus acting as a highly efficient photocatalyst. Nanoparticles also exhibited antilipolytic activity. Antibacterial potential was studied on four bacterial strains, viz. Escherichia Coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Staphylococcus mutans. For all the strains minimum inhibitory concentration (MIC) varied from 25 to 50 µg/ml.
Mehran Mirloei
University of Isfahan, Iran
Title: Rosmarinic acid, major polyphenol from Lemon balm (Melissa officinalis, L.) restrains non-enzymatic glycation of albumin
Time : 11:45-12:15
Biography:
Mehran Miroliaei is currently working as an Associate Professor Department of Biology, Faculty of Sciences, University of Isfahan, Iran.
Abstract:
Rosmarinic acid (RA) is a major component of medicinal plants such as Melissa officinalis. The present study demonstrates the protection of human serum albumin (HSA) from fructation at autoxidative and glycoxidation stage by (RA). Attenuation of Millard reaction measured by absorbance at the early stage of glycation, provided evidence for RA preventive role on HSA fructation. CD spectropolarimetry demonstrated that the transition of α to β conformer at the glycoxidation stage can be overcome by addition of RA. Moreover, fluorescent monitoring of advances glycation endproducts (AGE) formation at emission wavelength of 440 nm revealed that RA blocks the late stage of fructation. Amyloid conformers were found to be progressively generated during fructation as mesured by ThT fluorescence. Suppresion of conformational alterations induced by ROS production suggested that RA inhibits the formation of cross β-structures by modifying the transition of secondary and tertiary structures. The mechanism of RA action can be explained by the transistion metal ion chelating effect of RA in the oxidative reactions of AGE formation and/or by RA influence on the recations of dicarbonyl intermediates of AGE formation. The results indicate that the multi-target mode of RA action have promising potential for prevention of diabetic complications arising from HSA glyctation.
Birsen Demirata Ozturk
Istanbul Technical University, Turkey
Title: Detection and quantification of antibiotics residues in chicken meat by reversed-phase highperformance liquid chromatography
Time : 12:15-12:45
Biography:
Birsen Demirata Ozturk has obtained her PhD in 1986 and became Associate Professor in 1992 and full Professor in 2000 in the branch of Analytical Chemistry. Her research interest is in basic concepts of environmental and analytical chemistry and development of analytical methods for the spectrophotometric determination.
Abstract:
The purpose of this study is to analyze the effect of tetracycline and oxytetracycline antibiotics in chicken meat samples by High Performance Liquid Chromatography (HPLC) method. In addition, we will learn whether the antibiotic level is low according to MRL (maximum residue level) or not. In this study, penicillin G, tetracycline, oxytetracycline are chosen for their common objectionable usage in animals and for the difficulties in the procedure of analysis. We can find whether chickens were cut on time or not. The method involves the extraction of OTC from chicken meat and the determination by HPLC. Chicken meat which was purchased from different brand was analyzed by HPLC. We found different results according to chicken meat. We also found antibiotic residue in chicken which is fed in village. 37.6 μg of oxytetracycline residue was found in organic chicken. Normally tetracycline (TC) and oxytetracycline (OTC) levels in chicken breast won’t be above 100 μg per kg.
Suvarcha Chauhan
Himachal Pradesh University, India
Title: Conductometric and fluorescence probe analysis on molecular interactions between cationic surfactants in aqueous medium of glycyl dipeptide: Concentration and temperature effect
Time : 13:45-14:15
Biography:
Suvarcha Chauhan has completed her PhD in 1988 from Himachal Pradesh University, Shimla and worked as Post-doctoral Fellow at Department of Chemistry, Himachal Pradesh University, Shimla for 11 years and joined as Assistant Professor in the same department in 2001. She has published about 107 papers in reputed journals of national and international repute with 19 papers h-indexed and 46 papers i-10 indexed and has ~1200 citations to her credit.
Abstract:
The effect of cationic micelles of cetyltrimethylammonium bromide (CTAB) and dodecyltrimethylammonium bromide (DTAB) on interactions of glycyl dipeptide in aqueous medium have been studied in varying concentrations (0.001, 0.005 and 0.010 mol∙kg–1) at different temperatures (293.15 K to 293.15 K). The conductivity method is employed to determine critical micelle concentration, CMC i.e., point of aggregation and the results have been discussed in terms of glycylglycine–CTAB/DTAB hydrophobic and electrostatic interactions in aqueous medium. The obtained CMC values reveal the fact that the micellization tendency of the surfactant increases in the presence of glycyl dipeptide. The CMC’s of CTAB and DTAB have been found to decrease from 0.87 to 0.66 mmol∙kg–1 and 14.2 to 13.7 mmol∙kg–1 respectively as the [Glycyl dipeptide] increased from 0.001 to 0.01 mmol∙kg–1. The temperature dependence of the CMC values has been established in terms of ion–ion, ion–polar and hydrophobic–hydrophobic group interactions around the hydrophobic part of surfactants. Furthermore, the standard thermodynamic parameters of micellization have been evaluated and interpreted which enable to grasp fully the ion–ion/ion–hydrophilic interactions existing in the present ternary (surfactant–dipeptide–water) system. In addition, the pyrene fluorescence study has been used to study the change of micropolarity produced by the interactions of surfactants with glycyl dipeptide and the aggregation behaviour (CMC determination) of surfactants.
Dilek Ozyurt
Istanbul Technical University, Turkey
Title: HPLC–UV method development and validation for the determination of low level formaldehyde grown culture mushrooms in Turkey
Time : 14:15-14:45
Biography:
Dilek Ozyurt has completed her PhD from Istanbul Technical University in 2014 and received best PhD thesis award. She is a Research Chemist in the same university. Her research subject is determination of antioxidants method. She has published 14 papers in international journals.
Abstract:
Mushrooms are important nutritional source for people health. 73% of people consume mushroom in Turkey. Under favor of, climate and soil conditions, many of the mushroom kinds grow up in Turkey. Formaldehyde is used in some processes of mushroom agriculture and harvesting. These processes are incubation, sterilization of cover soil and reusage preparation processes of compost soil. Formaldehyde is colorless and burnable gas. International Agency on Cancer (IARC) categorizes formaldehyde as a group carcinogenic matter. In this work, formaldehyde amount analyzed by HPLC, originated from mushroom consumption. After the preparation of different concentrations formaldehyde solutions, calibration curve was created. Extract of muddy and clean mushrooms and washing water of mushrooms injected to HPLC with 2,4-Dinitrophenilhydrazin (DNPH) derivation. The amount of formaldehyde in samples calculated with using linear calibration graph and peak areas. After the calculations, the maximum concentration is 0.981±0.012 mg formaldehyde kg-1 wet mushroom and the minimum concentration is 0.309±0.017 mg formaldehyde kg-1 wet mushroom. Experimental outcomes compared with literature data and it shows they behave similar.
Mohammed Moayyad Shukr
University of Salahaddin, Iraq
Title: Determination of some heavy metals in blood serum of pregnant women who induced miscarriage using ICP technique
Time : 14:45-15:15
Biography:
My name Mohammed; I finished my B.Sc. degree at the age of 23 years from University of Salahaddin / College of Science / Department of Chemistry and my M.Sc. degree at the age of 29 at same university and same department. Now I am working as Chemist at clinical laboratory.
Abstract:
Introduction: Inductively coupled plasma - optical emission spectrometry (ICP – OES) is a powerful tool for the determination of metals in a variety of different sample matrices (1). Abortion is defined as the termination of a pregnancy resulting in or closely followed by the death of the embryo or fetus (2). It also called miscarriage which is the loss of the pregnancy prior to viability (before 22 weeks of pregnancy or less than 500 g) (3). Aim: The aim of this study was to determine the concentration levels of (arsenic, calcium and manganese) in blood serum of women who induced miscarriage in their first trimester (first 14 weeks of gestation) and healthy pregnant women with no history of miscarriage as control. Material and methods: Serum concentrations of heavy metals like (arsenic, calcium and manganese) were assayed using (ICP – OES) technique in (n = 50) patients (women who induced miscarriage) and (n = 15) healthy pregnant women (control). Results: Results were expressed as (Mean ± S.E.M.), the results showed that mean serum concentration levels of arsenic, calcium and manganese in patients were (0.0569 ± 0.0002), (5.547 ± 0.1033) and (0.0762 ± 0.00023) mg L-1 respectively, while in controls were (0.0371 ± 0.0009), (8.415 ± 0.1215) and (0.0783 ± 0.00025) mg L-1 respectively. Differences in serum arsenic, calcium and manganese between patients and controls were highly significant, (P value < 0.0001). Conclusion: The study showed that there was a highly significant reduction in serum levels of calcium and manganese in patients as compared to control group, while there was a highly significant increase in serum levels of arsenic in patients as compared to control group.
- Polymer Chemistry | Clinical Chemistry | Natural Chemistry
Location: ALGONQIN (A)
Chair
Jin Seok Lee
Sookmyung Womens University, South Korea
Co-Chair
Godwin Basil D Cunha
Cape Breton University, Canada
Session Introduction
Peng Ding
Shanghai University, P R China
Title: Highly thermal conductive composites with polyamide-6 covalently-grafted graphene by an in situ polymerization and thermal reduction process
Time : 11:45-12:15
Biography:
Peng Ding has completed his PhD in Polymer Chemistry and Physics from University of Science and Technology of China (USTC). His research interest is mainly focused on the Polymer Chemistry and Polymer Nanocomposites. He has published more than 50 papers, applied for 37 Chinese patents (17 authorized), and was awarded the First Shanghai Science and Technology Progress Prize and the Second Shanghai Science and Technology Progress Prize, China.
Abstract:
The thermal conductive polyamide-6/graphene (PG) composite is synthesized by in situ ring-opening polymerization reaction using ε-caprolactam as the monomer, 6-aminocaproic acid as the initiator and reduced graphene oxide (RGO) as the thermal conductive filler. The generated polyamide-6 (PA6) chains are covalently grafted onto graphene oxide (GO) sheets through the “grafting to” strategy with the simultaneous thermal reduction reaction from GO to RGO. The homogeneous dispersion of RGO sheets in PG composite favors the formation of the consecutive thermal conductive paths or networks at a relatively low GO sheets loading, which improves the thermal conductivity (λ) from 0.196 W•m−1•K−1 of neat PA6 to 0.416 W•m−1•K−1 of PG composite with only 10 wt% GO sheets loading.
Jin Seok Lee
Sookmyung Women’s University, South Korea
Title: Sequentially self-limited molecular layer deposition of uniformly aligned polyurea thin films
Time : 12:15-12:45
Biography:
Jin Seok Lee has completed his PhD from Sogang University and Post-doctoral studies from Harvard University, Department of Chemistry and Chemical Biology. He is an Associate Professor of Chemistry in Sookmyung Women’s University. He has published more than 45 papers in reputed journals.
Abstract:
Development of methods enabling the preparation of uniformly aligned polymer thin films at the molecular level is a prerequisite for realizing their optoelectronic characteristics as innovative materials; however, these methods often involve a compromise between scalability and accuracy. In this study, we have grown uniformly aligned polyurea thin films on a SiO2 substrate using molecular layer deposition (MLD) based on sequential and self-limiting surface reactions. By integrating plane-polarized Fourier-transform infrared, Raman spectroscopic tools and density functional theory (DFT) calculations, we demonstrated the uniform alignment of polyurea MLD films. Furthermore, the selective-wavelength absorption characteristics of these films were investigated by integrating optical measurements and finite-difference time-domain (FDTD) simulations of reflection spectra, resulting from their thickness-dependent fine resonance with photons.
Godwin Basil D’Cunha
Cape Breton University, Canada
Title: Phenylalanine/Tyrosine ammonia lyase enzyme catalyzed synthesis of the methyl ester of parahydroxycinnamic acid and its potential antibacterial activity
Time : 12:45: 13:15
Biography:
Godwin Basil D’Cunha completed his PhD in Biochemistry from The University of Mumbai, India in 1995 and did his Post-doctoral work in Protein Chemistry and Enzymology from 1995-1997 at The University of Mumbai. He relocated to USA in 1997 and was an Adjunct Assistant Professor (City University of New York, 1999 – 2001), and then relocated to Canada in 2001. He is an Associate Professor in the Department of Chemistry at Cape Breton University (CBU), Sydney, Nova Scotia, Canada (currently in his 14th year of service at CBU). His research group works on fundamental and applied aspects of Phenylalanine Ammonia Lyase (PAL), an enzyme with considerable medical, industrial, and biotechnological significance. He has published 13 papers in peer-reviewed reputed journals and has made 32 presentations of his work at national and international conferences.
Abstract:
Enzymes are molecular machines that are vital to sustain life in biological systems including humans. Enzyme catalysis has revolutionized manufacturing processes in pharmaceutical, chemical and food industries. We have shown that Phenylalanine Ammonia Lyase (PAL) enzyme functions efficiently in both aqueous and non-aqueous media. We have also successfully used PAL in the production of L-phenylalanine (L-Phe) and L-phenylalanine methyl ester (L-PM), fine chemicals with very high demand in chemical and food industries. Recently, we have successfully demonstrated Phenylalanine/tyrosine ammonia lyase (PTAL) catalyzed transformation of L-tyrosine methyl ester (L-TM) to para-hydroxycinnamic acid methyl ester (p-HCAM) and its antibiotic activity. Different conditions including pH, temperature, speed of agitating reaction milieu, enzyme concentration, and substrate concentration were optimized for the maximal formation of p-HCAM. The product (p-HCAM) was confirmed using Nuclear Magnetic Resonance spectroscopy (NMR). Fourier Transform Infra-Red spectroscopy (FTIR) was carried out to rule out potential hydrolysis of p-HCAM during overnight incubation. Potential antibacterial activity of p-HCAM was tested against several strains of Gram-positive and Gram-negative bacteria. In addition to using p-HCAM as an antibacterial agent (perhaps as a topical treatment agent or disinfectant), we also intend testing its potential applications as a food additive (inclusion in canned foods to prevent microbial contamination).
Abdalla H Karoyo
University of Saskatchewan, Canada
Title: Smart polymer materials - Tuning the physicochemical properties of polysaccharides via cross-linking conditions
Time : 14:00-14:30
Biography:
Abdalla H Karoyo obtained his PhD from the University of Saskatchewan under the supervision of Prof. Lee Wilson and P. Hazendonk (University of Lethbridge) in the 2014/2015 academic year. He has worked with Environment Canada as a Chemical Scientist and is currently working with Prof. Wilson as a Post-doctoral fellow.
Abstract:
The physicochemical properties (e.g. surface chemistry and solubility) of polysaccharide-based polymers can be tuned via cross-linking conditions. The structure and function of novel urethane-based polymer materials containing 1,6-hexamethylene diisocyanate (HDI) and ï¢- cyclodextrin ï¢-CD) in a 1:1, 3:1, and 6:1 (HDI:β-CD) mole ratios (denoted HDI-1, -3, and -6, respectively) were studied. The host-guest chemistry and adsorption properties of the HDI-polymers vary according to the accessibility of the cavity inclusion sites of β-CD, the surface chemistry of the non-inclusion domains of the polymer framework, and the nature of the guest. On one extreme, HDI-1 with the lowest cross-linker content is a water soluble linear polymer with ~100% inclusion site accessibility and a behavior that is characteristic of a “smart” material. The HDI-1 polymer herein adopts a compact and extended conformation as a function of temperature change and/or guest concentration gradient. On the other extreme, HDI-6 with the highest cross-linker content is a water insoluble branched polymer with negligible inclusion sites accessibility and readily available non-inclusion domains. The adsorption of the HDI-polymers for the perfluorocarbon and hydrocarbon guests occur within the non-inclusion sites, as well as within the inclusion sites in the absence of steric hindrance; whereas, the removal capacity meets or exceeds literature values. The molecular structure of the HDI-polymers was investigated using such techniques as Raman, 1D/2D 1H NMR, and circular dichroism spectroscopy.
MarÃa Belén Camarada
Universidad Bernardo O´Higgins, Chile
Title: Chemical and electrochemical synthesis of graphene/conducting polymers nanocomposites
Time : 14:30-15:00
Biography:
María Belén Camarada has completed her PhD from Pontificia Universidad Católica de Chile. She is a member of the research team of Laboratorio de Bionanotecnología, Universidad Bernardo O´Higgins, Chile, focusing on the development of electrochemical DNA sensors. She has participated in national and international conferences and has ISI publications in the area of Electrochemistry and Computational Simulations.
Abstract:
Potentiometric, amperometric and conductometric electrochemical sensors have been widely developed as an inexpensive and simple method to sensitively detect a variety of analytes in the areas of environmental, industrial, and clinical analyses. Among new interfaces that have been tested for electrochemical sensors, carbon nanomaterials have been reported as advantageous because they increase the electro-active surface area, enhance electron transfer, and promote adsorption of molecules. Graphene, a two-dimensional single layer of graphite and one-atom-thick sheet material has received increasing attention due to its unique physicochemical properties such as large surface area, excellent conductivity and strong mechanical strength. Recently, Conducting Polymers (CP) have been applied as materials to modify the electrode surface and has been demonstrated that carbon materials can reinforce the stability of CP and provide more active nucleation sites in electrochemical sensors. In this work, different nanocomposites of graphene and CP: Poly(aniline), poly(pyrrole) and poly(thiophene), were synthesized through chemical synthesis using a salt as oxidant and also through in situ electrochemical polymerization in the presence of graphene oxide. Conductivity and stability of the new materials synthesized by both pathways were compared electrochemically, while morphologies and structure were analyzed by AFM, FT-IR and UV-Vis. Results provided relevant information about the best route of synthesis of nanocomposites applied in electrochemical sensors.
Tulio Chavez-Gil
Coppin State University, USA
Title: Bio-inorganic non lactamase metallo antibiotics
Time : 15:00-15:30
Biography:
Tulio Chavez-Gil is currently working as an Assistant Professor of Chemistry at Coppin State University, Baltimore, MD. He got his BS in Chemistry at Universidad del Valle (Cali, Colombia) where he worked as Researcher Assistant designing the Coals and Petroleum Lab in the School of Engineering. He earned his PhD in Inorganic Chemistry at Universidade de São Paulo, (São Paulo, BR) in 1997. He spent 2 years (1997-1999) as Post-doctoral fellow at University of Kumamoto (Japan) and other 2 (2000-2002) at University of Puerto Rico - Mayaguez. His academic accomplishments include positions at Universidad de Los Andes (Bogota, Col - 2003), Inter-American University of Puerto Rico (2004-2014). He has authored/coauthored 27 peer-reviewed publications (5 in Geology), one patent application and more than 70 research/educational presentations. He has been awarded with the Cnpq scholarship award (BR), the Japan Society for the Promotion of Science (JSPS), the MBRS-NIH award (UPR), and the Ronald E McNair mentorship award 2007-2014 at IAUPR. He is serving as an Editorial Board Member for the Structural Chemistry & Crystallography Communication Journal.
Abstract:
The fast emerging in antimicrobial resistance has been the timely challenge for all classes of antibiotics, temporarily assuaging the concerns of modern medicine. Nowadays, there has been a significant retraction on the drugs design and research investment to attain new antimicrobial medicines by the major pharmaceutical companies with the coinciding escalation in global nosocomial infection. Metallo-antibiotic compounds has been less related with medicine applications and here we are presenting new results about the antimicrobial activity of a series of chelators having N and O functionalities and its vanadium complexes as a lane of research developed with particular emphasis to test its antibiotic activity against the emergent so called “ESKAPE” super bugs. Some of the most serious infections caused by ESKAPE strains are bateremia, pneumonia, osteomyelitis, acute endocarditis, myocarditis, pericarditis, cerebritis, meningitis, chorioamnionitis, scalded skin syndrome, abscesses of the muscle, urogenital tract, central nervous system, and various intra abdominal organs. The proposed artificial antibiotics and its derived complexes have being synthesized between dipicolonic acid (found in bacteria’s cell wall), 2-methylsalycilate, anthranilic acid, and NH4VO3. Those non-ï¢-lactamase chelators and its vanadium compounds, are still acting as either cytotoxic or bacteriostatic agents against a broad scope of bacterial strains. The in vitro preliminary screening with Gram-(positive/negative) strains suggests powerful growth inhibition activity on different bacteria viz., Staphylococcus aureus; Staphylococcus epidermidis; Bacillus cereus; Streptococcus faecalis; Acinetobacter baumannii; Citrobacter freundii; Salmonella typhimurium; Serratia marcescens; Escherichia coli; Enterobacter aerogenes; Enterobacter cloacae; Klebsiella pneumoniae; Pseudomonas aeruginosa, and Proteus vulgaris.