Klimesová Vera, Zahajská Lenka, Waisser Karel, Kaustová Jarmila, Möllmann Ute
Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, 50005 Hradec Králové, Czech Republic.
Farmaco. 2004 Apr;59(4):279-88. doi: 10.1016/j.farmac.2004.01.006.
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.
通过起始的三唑-3-硫醇与适当取代的苄基卤进行烷基化反应，合成了一系列1,2,4-三唑和4-甲基-1,2,4-三唑的3-苄基硫烷基衍生物。对该系列的所有成员进行了针对结核分枝杆菌、鸟分枝杆菌和两株堪萨斯分枝杆菌的体外抗分枝杆菌活性评估。活性以最低抑菌浓度表示。这些化合物仅表现出中等或轻微的抗分枝杆菌活性。最低抑菌浓度范围为32->1000微摩尔/升。活性最高的物质在苄基部分带有两个硝基或一个硫代酰胺基团。至于细胞毒性作用，所评估的化合物可被认为具有中等毒性。
