ANTI-BACTERIAL ACTIVITY OF THIOL-SUBSTITUTED 1,3,4- OXADIAZOLES - Swaminathan, Gomathi;NS, Roshan;Raman, Kannan
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The main objective of the research is to design an active thiol substituted oxadiazole inhibitor against GlmS receptor of gram-negative and gram-positive bacteria with in silico and in vitro antibacterial approaches. A scaffold of 1,3,4-oxadiazole was designed and the synthetic feasibility to attain the scaffold. PyRx software was used. The ligand poses with the least free energy. ADMET studies were conducted. The synthesis steps included 4 different reactions. Substituted carboxylic acids were used as the starting reagent. All of the reactions were monitored by TLC. Synthesized compounds were…mehr

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Produktbeschreibung
The main objective of the research is to design an active thiol substituted oxadiazole inhibitor against GlmS receptor of gram-negative and gram-positive bacteria with in silico and in vitro antibacterial approaches. A scaffold of 1,3,4-oxadiazole was designed and the synthetic feasibility to attain the scaffold. PyRx software was used. The ligand poses with the least free energy. ADMET studies were conducted. The synthesis steps included 4 different reactions. Substituted carboxylic acids were used as the starting reagent. All of the reactions were monitored by TLC. Synthesized compounds were characterized using FT-IR and MASS spectra. The in vitro antibacterial activity of the compounds was examined and evaluated by minimum inhibitory concentration studies. From MIC study results, out of all the compounds, NOV-4 showed considerable antibacterial activity against the resistant strain of MRSA (43300) with a MIC of 4.77µg/L far bettering the MIC of the standard which was a moderate 209.24 µg/L. From these results, it is concludable that the designed scaffold shows significant inhibitory action against the GlmS receptor protein.
Autorenporträt
Dr. Gomathi Swaminathan, working as a Lecturer in the Department of Pharmaceutical Chemistry, JSS College of Pharmacy, JSS Academy of Higher Education and Research, Ooty, Nilgiris, Tamil N¿du, India. She has received a research grant from ICMR, New Delhi, and a seminar grant from SERB-DST and CSIR, New Delhi.