| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1394191 | European Journal of Medicinal Chemistry | 2014 | 13 Pages |
•Synthesis of 7-piperazinylquinolones–tetrazole derivatives via using Ugi-4CC.•Some of synthesized derivatives showed excellent antibacterial activity.•These compounds displayed no toxicity against mammalian cell line L-929.•It is a successful approach to overcome the problem of resistance.
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 S. 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.
Graphical abstractA new class of 7-piperazinylquinolone–tetrazole derivatives were synthesized via using Ugi-4CC reaction. Most of the synthesized compounds exhibited potent antibacterial activity against various strains of Staphylococcus aureus. Figure optionsDownload full-size imageDownload as PowerPoint slide
