Pyridoquinolones containing azetidinones: synthesis and their biological evaluation

Abstract

A series of pyridoquinolone 4-oxo-1,4-dihydro(4′-methyl-6′-chloropyrido[2,3-h])quinoline-3-[N-(substituted phenyl methylidine)]carbohydrazide 3a–j and 4-oxo-1,4-dihydro(4′-methyl-6′-chloropyrido[2,3-h])-3-[N-{(3-chloro-2-oxo-4-(substituted phenyl) azetidine-1-yl)amino}carbonyl] quinoline 4a–j have been synthesized via 4-oxo-1,4-dihydro-(4′-methyl-6′-chloropyrido[2,3-h])quinoline carboxylate 1. All the compounds were proved by IR, 1H-NMR, 13C-NMR spectral studies and elemental analysis. Antibacterial activities (MIC) against E. coli, P. aeruginosa, S. aureus and S. pyogenes, and antifungal activities against C. albicans, A. niger and A. clavatus were screened, whereas selected compounds were screened against Mycobacterium tuberculosis H37Rv and compared with standard drugs.