1,2,3-Triazole fused with pyridine/pyrimidine as new template for antimicrobial agents: Regioselective synthesis and identification of potent N-heteroarenes

The 1,2,3-triazole fused pyridine/pyrimidine derivatives were synthesized and evaluated as new and potential antimicrobial agents. [Display omitted] •Explored 1,2,3-triazolo pyridine/pyrimidine as new template for antimicrobial agents.•Demonstrated the application of Buchwald’s strategy to N-heteroarene system.•Two compounds were comparable to streptomycin and several were comparable to mancozeb. The 1,2,3-triazole ring fused with pyridine/pyrimidine was explored as new template for the identification of potential antimicrobial agents. The regioselective synthesis of these pre-designed N-heteroarenes was achieved via exploring the application of Buchwald’s strategy (i.e. C–N bond formation/reduction/diazotization/cyclization sequence) to the N-heteroarene system. Two of them showed promising antibacterial (comparable to streptomycin) and several showed potent antifungal (comparable to mancozeb) activities.