Abstract
A small library of novel pyrazolyl-imidazole-triazole hybrids (3a-3r) has been designed and synthesized based on hybrid pharmacophore approach using click reaction of N-propargylated pyrazolyl-imidazole (1) with several aryl azides carrying different substituents. The hybrids were characterized by different spectral techniques like IR, 1H, 13C NMR, HRMS and X-ray crystallography. ADME profile was assessed for these derivatives to get an insight on their pharmacokinetic/dynamic attributes. The synthesized hybrids were screened for antimicrobial activities against bacterial and fungal strains. Hybrid 3o and 3k demonstrated broad spectrum antibacterial activity against all tested bacterial strains except S. aureus and even better than clinically approved drug Norfloxacin. Hybrids 3c (MIC, 0.0082 µmol/mL), 3d (MIC, 0.0075 µmol/mL), 3e (MIC, 0.0077 µmol/mL) and 3m (MIC, 0.0081 µmol/mL) showed more than two-fold inhibitory efficacy against C. albicans while against A. niger, 3c (MIC, 0.0082 µmol/mL) showed five-fold inhibitory efficacy as compared with Fluconazole. Moreover, in-silico molecular docking study investigated on E. coli topoisomerase-II DNA gyrase revealed a good binding interaction with most potent hybrids 3o and 3k.
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