ANTI-BACTERIAL ACTIVITY OF THIOL-SUBSTITUTED 1,3,4- OXADIAZOLES. EVALUATION OF SOME NOVEL THIOL-SUBSTITUTED 1,3,4- OXADIAZOLES AS GlmS INHIBITORS

      Аннотация: 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.

Ключевые слова: OXADIAZOLE, Anti-Bacterial, Synthesis, charaterization, in vitro