4.7 Article

Synthesis and in vitro antibacterial evaluation of N-[5-(5-vitro-2-thienyl)-1, 3,4-thiadiazole-2-yl] piperazinyl quinolones

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EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 38, 期 9, 页码 851-854

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ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/S0223-5234(03)00148-X

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quinolones; 5-nitrothiophene; synthesis; antibacterial activity

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A series of N-[5-(5-vitro-2-thienyl)-1,3,4-thiadiazole-2-yl]piperazinyl quinolones (7a-c) were synthesized and evaluated for in vitro antibacterial activity against some Gram-positive and Gram-negative bacteria. The antibacterial data revealed that compounds 7a-c had strong and better activity against tested Gram-positive organisms than the reference quinolones such as ciprofloxacin, norfloxacin and enoxacin. However, all three compounds were nearly inactive against Gram-negative bacteria. Compound 7a (ciprofloxacin analogue) was the most active compound against Gram-positive bacteria (MIC=0.008-0.015 mug mL(-1)). (C) 2003 Editions scientifiques et medicales Elsevier SAS. All rights reserved.

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