No abstract

: Some phenyl substituted thiazole linked 1, 2, 4- triazole derivatives (8a-8j) were synthesized and elucidated their structures using different spectroscopic data of IR, 1HNMR, 13CNMR & mass spectroscopy. These synthesized derivatives were evaluated for their antibacterial activity using broth dilution assay. Further, mechanism of action of test compounds was examined using protein leakage assay. Amongst all compound 8c showed most potent activity with lowest IC50 values 180 μM and 120 μM against S. aureus & B. cereus respectively whereas compound 8j demonstrated strong inhibitory activities only against negative strains P. aeruginosa and E. coli with lowest IC50 values 240 μM and 200μM respectively.

A novel series of phenyl substituted azetidine containing 1, 2, 4‐triazole derivatives 7(a–j) were synthesized and characterized by IR, 1HNMR, 13CNMR, and mass spectroscopy. Synthesized 1, 2, 4‐triazole derivatives were subsequently assayed in vitro to investigate their antibacterial activity against Staphylococcus aureus, Pseudomonas aeruginosa, and Escherichia coli using broth dilution method. Compounds 7c, 7d, and 7e exhibited potent inhibitory activities as compared to standard cefotaxime. Further, fluorescence spectral studies were also carried out to ascertain the antibacterial potential of compound 7c against two bacterial strains, that is, P. aeruginosa and S. aureus. In docking studies, all the compounds exhibited good docking scores between −12.04 and −11.36 kcal/mol and indicated that compounds could act through inhibition of bacterial DNA gyrase (PDB ID 3U2D). Among all, 7c has shown the maximum docking score and found in agreement to in vitro studies. In conclusion, synthesized 1, 2, 4‐triazole derivatives holds substantial caliber to be categorized as antibacterial agents.