Investigation of Ugi-4CC derived 1H-tetrazol- 5-yl-(aryl) methyl piperazinyl-6-fluoro-4-oxo-1, 4-dihydroquinoline-3-carboxylic acid: Synthesis, Biology and 3D-QSAR Analysis

Abstract

Novel series of 7-piperazinylquinolones with tetrazole derivatives were synthesized and evaluated for their antibacterial activity against various strains of Staphylococcus aureus. All the synthesized compounds showed significant in vitro antibacterial activity against Gram-positive bacteria whereas some compounds displayed moderate activity against Gram-negative bacteria. Among all the synthesized compounds, compounds (6a-c, 6e-g, 6i-k, 6m, 6’f and 6’m) were found to be more effective with MIC ranging from (0.78-3.12 µg/mL) against Staphylococcus aureus (ATCC-29213) than the control; ciprofloxacin (MIC = 25 µg/mL). Moreover, these analogues displayed no toxicity up to MIC = 0.39 µg/mL against mammalian cell line L-929. Furthermore, to correlate the biological activities of synthesized compounds with their 3D conformation, we attempted 3D-QSAR study.