Navarrete-Vázquez Gabriel, Yépez Lilián, Hernández-Campos Alicia, Tapia Amparo, Hernández-Luis Francisco, Cedillo Roberto, González José, Martínez-Fernández Antonio, Martínez-Grueiro Mercedes, Castillo Rafael
Departamento de Farmacia, Facultad de Química, UNAM, CU, DF 04510, Mexico.
Bioorg Med Chem. 2003 Oct 15;11(21):4615-22. doi: 10.1016/s0968-0896(03)00497-8.
Albendazole (Abz) and Mebendazole (Mbz) analogues have been synthesized and in vitro tested against the protozoa Giardia lamblia, Trichomonas vaginalis and the helminths Trichinella spiralis and Caenorhabditis elegans. Results indicate that compounds 4a, 4b (Abz analogues), 12b and 20 (Mbz analogues) are as active as antiprotozoal agents as Metronidazole against G. lamblia. Compound 9 was 58 times more active than Abz against T. vaginalis. Compounds 8 and 4a also shown high activity against this protozoan. Compounds 4b and 5a were as active as Abz. None of the Mbz analogues showed activity against T. vaginalis. The anthelmintic activity presented by these compounds was poor.
已合成阿苯达唑（Abz）和甲苯达唑（Mbz）类似物，并针对原生动物蓝氏贾第鞭毛虫、阴道毛滴虫以及蠕虫旋毛虫和秀丽隐杆线虫进行了体外测试。结果表明，化合物4a、4b（阿苯达唑类似物）、12b和20（甲苯达唑类似物）作为抗原生动物药物，对蓝氏贾第鞭毛虫的活性与甲硝唑相当。化合物9对阴道毛滴虫的活性比阿苯达唑高58倍。化合物8和4a对这种原生动物也表现出高活性。化合物4b和5a与阿苯达唑活性相当。没有一种甲苯达唑类似物对阴道毛滴虫表现出活性。这些化合物的驱虫活性较差。
