NEW GROUPS OF POTENTIAL ANTITUBERCULOTICS - 5-ALKYLTHIO-1-ARYLTETRAZOLES

A series of 5-alkylthio-1-aryltetrazoles 1-14 was prepared by alkylati on of the corresponding 1-aryltetrazole-5-thiols with alkyl bromides i n the cyclohexane-aqueous potassium hydroxide system. The new compound s were evaluated for their activity against Mycobacterium tuberculosis , M. kansasii, M. avium and M. fortuitum. The effects of aryl and alky l fragments on minimum inhibitory concentrations (MIC) against M. tube rculosis and M. kansasii were analyzed by Free-Wilson method. On basis of calculated fragment contributions, 5-butylthio-1-(3,4-dimethylphen yl)tetrazole (15) was predicted to be the most antimycobacterially act ive derivative in the present series studied and its activity was veri fied 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. kansasi i, respectively.