Navarrete-Vázquez G, Cedillo R, Hernández-Campos A, Yépez L, Hernädez-Luis F, Valdez J, Morales R, Cortés R, Hernández M, Castillo R
Departamento de Farmacia, Facultad de Química, UNAM, CU, Mexico D.F.
Bioorg Med Chem Lett. 2001 Jan 22;11(2):187-90. doi: 10.1016/s0960-894x(00)00619-3.
2-(Trifluoromethyl)benzimidazole derivatives substituted at the 1-, 5-, and 6-positions have been synthesized and in vitro tested against the protozoa Giardia lamblia, Entamnoeha histolytica. and the helminth Trichinella spiralis. Results indicate that all the compounds tested are more active as antiprotozoal agents than Albendazole and Metronidazole. One compound (20) was as active as Albendazole against T. spiralis. These compounds were also tested for their effect on tubulin polymerization and none inhibited tubulin polymerization.
已合成了在1、5和6位被取代的2-（三氟甲基）苯并咪唑衍生物，并针对原生动物贾第鞭毛虫、溶组织内阿米巴以及蠕虫旋毛虫进行了体外测试。结果表明，所有测试化合物作为抗原生动物药物比阿苯达唑和甲硝唑更具活性。一种化合物（20）对旋毛虫的活性与阿苯达唑相当。还测试了这些化合物对微管蛋白聚合的影响，结果显示它们均未抑制微管蛋白聚合。
