Design and Synthesis, Biological Evaluation of Bis-(1,2,3- and 1,2,4)-Triazole Derivatives as Potential Antimicrobial and Antifungal Agents

Bioorg Med Chem Lett. 2021 Mar 31:128004. doi: 10.1016/j.bmcl.2021.128004. Online ahead of print.


A new series of bis-1,2,3- and 1,2,4-triazoles (10a-m) were designed and efficiently synthesized using methyl salicylate as a starting material as potential antimicrobial agents. All compounds were characterized by their proton &13C NMR, IR, Mass spectral data, and elemental analysis. The final compounds 10a-m were in vitro screened for antimicrobial and antifungal activity against gram negative Pseudomonas aeruginosa, Escherichia coli, gram positive Bacillus subtilis, Staphylococcus aureus strains and Aspergillus niger &Saccharomyces cerevisiae. Majority of the synthesized compounds were exhibited potent antimicrobial activity (MIC 3.9 µg/mL) and promising antifungal activity with the zone of inhibition (ZOI) 1.5-8.2 mm. Compounds like 10d and 10f exhibited best antimicrobial activity against S. aureus. The molecular docking analysis revealed that all the synthesized derivatives shown better binding affinities. Among all, compound 10f exhibited best scores. Hence, there was an assumption that introduction of para-chloro and bromo-phenyl aromatic groups on triazole moiety could result excellent antimicrobial activity. This substantial growth inhibitory activity of bis-1,2,3- and 1,2,4-triazole derivatives suggested these compounds could assist a new way in the development of lead molecules against microbial infection and antimicrobial resistance investigations.

PMID:33811989 | DOI:10.1016/j.bmcl.2021.128004

Source: Industry