Synthesis and antimycobacterial activity of 1,2,4-triazole 3-benzylsulfanyl derivatives.
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.
Klimesová
Vera
V
Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, 50005 Hradec Králové, Czech Republic. klimeso@faf.cuni.cz
Zahajská
Lenka
L
Waisser
Karel
K
Kaustová
Jarmila
J
Möllmann
Ute
U
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D008698:Mesylates / Q000138:chemical synthesis* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests / Q000706:statistics & numerical data; D009162:Mycobacterium avium / Q000187:drug effects / Q000254:growth & development; D019909:Mycobacterium kansasii / Q000187:drug effects / Q000254:growth & development; D009169:Mycobacterium tuberculosis / Q000187:drug effects / Q000254:growth & development; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D008698:Mesylates; D014230:Triazoles; C035617:phenylmethanesulfonic acid