Conformationally Constrained Analogs of N‐Substituted Piperazinylquinolones: Synthesis and Antibacterial Activity of N‐(2,3‐Dihydro‐4‐hydroxyimino‐4H‐1‐benzopyran‐3‐yl)‐piperazinylquinolones |
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| Authors: | Saeed Emami Alireza Foroumadi Nasrin Samadi Mohammad A. Faramarzi Saeed Rajabalian |
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| Affiliation: | 1. Pharmaceutical Sciences Research Center, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran;2. Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran;3. Faculty of Pharmacy and Pharmaceutics Sciences Research Center and Kerman Neuroscience Research Center, Kerman University of Medical Sciences, Kerman, Iran;4. Department of Pharmaceutical Biotechnology, Biotechnology Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran |
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| Abstract: | A series of novel quinolone agents bearing a particular bulky and conformationally constrained bicyclic substituent (2,3‐dihydro‐4‐hydroxyimino‐4H‐1‐benzopyran‐3‐yl‐ moiety) on the piperazine ring of 7‐piperazinyl quinolones (norfloxacin, enoxacin, ciprofloxacin, and levofloxacin) were synthesized and evaluated against a panel of Gram‐positive and Gram‐negative bacteria. Among these derivatives, ciprofloxacin counterpart 9c , highly inhibited the tested Gram‐positive bacteria, superior to that of the reference drugs, and displayed antibacterial activity at non‐cytotoxic concentrations. |
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| Keywords: | Antibacterial activity Conformationally constrained analogs 2,3‐Dihydro‐4H‐1‐benzopyran Quinolones |
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