Author:
Waisser Karel,Kuneš Jiří,Hrabálek Alexandr,Macháček Miloš,Odlerová Želmíra
Abstract
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 μmol l-1 and 61 μmol l-1 were obtained for its activity against M. tuberculosis and M. kansasii, respectively.
Publisher
Institute of Organic Chemistry & Biochemistry
Cited by
14 articles.
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