New benzimidazole derivatives as antimycobacterial agents

被引:57
作者
Klimesová, V
Kocí, J
Waisser, K
Kaustová, J
机构
[1] Charles Univ Prague, Fac Pharm, Dept Inorgan & Organ Chem, Hradec Kralove 50005, Czech Republic
[2] Reg Inst Hyg, Natl Reference Lab Mycobacterium Kansasii, Ostrava 72892, Czech Republic
来源
FARMACO | 2002年 / 57卷 / 04期
关键词
antimycobacterial activity; 2-alkylsulfanyl derivatives; 5-methylbenzimidazole-2-thiol; Mycobacterium tuberculosis; nontuberculous mycobacteria;
D O I
10.1016/S0014-827X(02)01218-1
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
A set of 2-alkylsulfanyl derivatives of 5-methylbenzimidazole was synthesized and evaluated for antimycobacterial activity. The structures of the compounds were confirmed by H-1 NMR and IR data, and their purity by elemental analysis. Antimycobacterial activities against Mycobacterium tuberculosis and nontuberculous mycobacteria were expressed as the minimum inhibitory concentration. The substances exhibited significant antimycobacterial activity, in particular against both strains of Mycobacterium kansasli. The effect of the most active compound in the set, 3,5-dinitro derivative 3t, exceeded that of the standard isoniazide against M. kansasii and Mycobacterium avium. (C) 2002 Editions scientifiques et medicales Elsevier SAS. All rights reserved.
引用
收藏
页码:259 / 265
页数:7
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