| Popis: |
Newer antibacterial agents are needed to combat the growing bacterial infections. Triazoles are one of the leading and most sought out nucleus amongst the heterocyclic rings in the drug world. 1, 2, 3-Triazoles are synthesized by Click Chemistry of alkynes with azides. A synergistic effect is observed when the triazoles are combined with other heterocycles. They also exhibit diversified therapeutic activities like anti-viral, anti-bacterial, anti-diabetic, anti-tubercular, anti-inflam-matory, antihypertensive etc which makes Triazoles an interesting molecule for the researchers to work on. In the current study, we combined 1,2, 3-triazoles with thiophene ring system to get synergistic antibacterial activity. Here, 12 derivatives of 4, 5-substituted-1, 2, 3-Triazoles were subjected to in silico docking studies on Biotin ligase protein (PDB ID: 3V7R). The compounds that showed the best results were synthesized. The newly synthesized derivatives were characterized by using IR, H1 NMR and Mass spectrum. All the synthesized derivatives were evaluated for antibacterial activity against Gram-negative bacteria (E. coli and P. aerugenosa) and gram-positive bacteria (B. subtilis and S. aureus). The compounds showed moderate to good activity, which was comparable to that of the standard Streptomycin drug. |
