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

被引:188
作者
Foroumadi, A
Mansouri, S
Kiani, Z
Rahmani, A
机构
[1] Kerman Univ Med Sci, Fac Pharm, Dept Med Chem, Kerman, Iran
[2] Kerman Univ Med Sci, Fac Med, Dept Microbiol, Kerman, Iran
关键词
quinolones; 5-nitrothiophene; synthesis; antibacterial activity;
D O I
10.1016/S0223-5234(03)00148-X
中图分类号
R914 [药物化学];
学科分类号
100701 [药物化学];
摘要
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.
引用
收藏
页码:851 / 854
页数:4
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