New groups of potential antituberculotics: 5-alkylthio-1-aryltetrazoles

被引：15

作者：

Waisser, K ^{[1
]}

Kunes, J ^{[1
]}

Hrabalek, A ^{[1
]}

Machacek, M ^{[1
]}

Odlerova, Z ^{[1
]}

机构：

[1] INST PREVENT & CLIN MED,BRATISLAVA 83301,SLOVAKIA

来源：

COLLECTION OF CZECHOSLOVAK CHEMICAL COMMUNICATIONS | 1996年 / 61卷 / 05期

关键词：

5-alkylthio-1-aryltetrazoles; antituberculotics; phase-transfer catalysis; structure-activity relationships;

D O I：

10.1135/cccc19960791

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A series of 5-alkylthio-1-aryltetrazoles 1-14 was prepared by alkylation of the corresponding 1-aryltetrazole-5-thiols with alkyl bromides in the cyclohexane-aqueous potassium hydroxide system. The new compounds were evaluated for their activity against Mycobacterium tuberculosis, M. kansasii, M. avium and M. fortuitum. The effects of aryl and alkyl fragments on minimum inhibitory concentrations (MIC) against M. tuberculosis and M. kansasii were analyzed by Free-Wilson method. On basis of calculated fragment contributions, 5-butylthio-1-(3,4-dimethylphenyl)tetrazole (15) was predicted to be the most antimycobacterially active derivative in the present series studied and its activity was verified experimentally. MIC values of 30 mu mol l(-1) and 61 mu mol l(-1) were obtained for its activity against M. tuberculosis and M. kansasii, respectively.

引用

页码：791 / 798

页数：8

共 17 条

[1] TUBERCULOSIS - BACK TO A FRIGHTENING FUTURE [J].