New 2-Phenylquinoline-Based Bis-Methoxymethyl-1,2,3-Triazoles as Potential Antimicrobial Agents: Synthesis and Molecular Docking Studies against COVID-19

摘要

Synthesis of novel 2-phenylqinoline conjugated bis-triazole analogues 8(a-n) demonstrated by a series of reactions concerning Vilsmeier-Haack reaction, Suzuki-Miyaura cross coupling, reduction of carbonyl groups, and click reaction. The structure of final compounds predicted based on IR, H-1, C-13 NMR and Mass spectral data analysis. The title compounds were screened for their in vitro antimicrobial activities against two-gram positive (S. aureus and S. pyogens) and two-gram negative (P. aeruginosa and E. coli) bacteria, and two fungal strains (S. rolfs and F. ricini) by employing Amoxicillin and Bavistin as standard drugs, respectively. The compound containing 3-chlorophenyl, 4-(trifluoromethyl)phenyl, 3,4-dimethylphenyl and 3-fluoro-4-chlorophenyl residues, indicated promising antibacterial activity and the best antifungal activity was reported for compounds containing 3-chlorophenyl, 4-methoxyphenyl and 4-(trifluoromethyl)phenyl residues. Further, Insilco screening of these compounds against COVID-19 main protease of corona virus had displayed good docking scores and binding interactions in its active site pocket.