Synthesis of novel triazole functionalized pyridine derivatives as potential antimicrobial and anti-biofilm agents

A series of novel 1-substituted (1H-1,2,3-triazole-4-yl) methoxy functionalized pyridine derivatives 5 and 6 have been prepared starting from 2(1H) pyridone 1 via selective O-propargylation followed by reaction with diverse substituted azides under Sharpless conditions. All the compounds 5 and 6 have been screened for antimicrobial activity, minimum bactericidal concentration and biofilm inhibition activity. Compounds 5d, 5I and Ss which showed promising activity specifically towards Staphylococcus aureus MTCC 96 and Staphylococcus aureus MLS-16 MTCC 2940 have been identified. Further, in silico docking studies have been carried out on the inhibition of dehydrosqualene synthase enzyme of S. aureus. This is a key enzyme in the biosynthesis of staphyloxanthin, a virulence factor for S. aureus. Further, on screening for antioxidant activity, the compounds 5I(,) 5q and 5n showed promising activity.