Il Farmaco 2004-04-01

Synthesis and antimycobacterial activity of 1,2,4-triazole 3-benzylsulfanyl derivatives.

Vera Klimesová, Lenka Zahajská, Karel Waisser, Jarmila Kaustová, Ute Möllmann

Index: Il Farmaco 59(4) , 279-88, (2004)

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Abstract

Series of 3-benzylsulfanyl derivatives of 1,2,4-triazole and 4-methyl-1,2,4-triazole were synthesized by alkylation of starting triazole-3-thiol with appropriately substituted benzyl halide. All members of the set were evaluated for in vitro antimycobacterial activity against Mycobacterium tuberculosis, M. avium, and two strains of M. kansasii. The activities were expressed as the minimum inhibitory concentration. The compounds exhibited only a moderate or slight antimycobacterial activity. Minimum inhibitory concentrations fall into a range of 32->1000 micromol/l. The most active substances bear two nitro groups or a thioamide group on the benzyl moiety. As regards the cytotoxicity effect, the evaluated compounds can be considered as moderately toxic.