Design, Synthesis, Docking, Characterization and Biological Screening of Novel Azetidinone Derivatives of Nicotinic Acid

Abstract

Background:The prevailing multiple drug resistance among the bacterial species is alarmingly rising day to day, becoming a global threat. Many infectious diseases have become untreated due to the development of resistance in bacterial species, which have a considerable impact on mortality.Methods:In this present study, we aimed to synthesize a series of 12 compounds [S1-S12], which are azetidinone derivatives of nicotinic acid. The in vitro antibacterial studies were performed against certain species of gram-negative and gram-positive bacteria. Molecular docking studies were performed to identify the affinity towards the target protein. The antioxidant study was also performed for the synthesized compounds.Results:All the synthesized compounds exhibited moderate to potent antibacterial activity with a MIC range of 9.8-21.6 μgmL-1, compounds were active against all tested micro-organisms. The compounds substituted with electron-donating groups like hydroxyl showed higher antioxidant activity compared to others. Docking studies were performed on the active site of DNA gyrase [PDBID: 5L3J,2XCT, 1W7Q].Conclusion:The present study reveals that the compounds synthesized exhibit very good antimicrobial activity and antioxidant activity. Therefore, these compounds may be used as a lead for the anticancer, anti-tubercular and other chemotherapeutic agents in future studies.