K. Waisser et al., NEW GROUPS OF POTENTIAL ANTITUBERCULOTICS - 5-ALKYLTHIO-1-ARYLTETRAZOLES, Collection of Czechoslovak Chemical Communications, 61(5), 1996, pp. 791-798
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.