Synthesis and antiparasitic activity of albendazole and mebendazole analogues.
Synthesis and antiparasitic activity of albendazole and mebendazole analogues.
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DOI：
10.1016/s0968-0896(03)00497-8
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发表时间：
2003-10
影响因子：
3.5
通讯作者：
Gabriel Navarrete-Vázquez;Lilián Yépez;A. Hernández-Campos;A. Tapia;F. Hernández‐Luis;R. Cedillo;
中科院分区：
文献类型：
--
作者：
Gabriel Navarrete-Vázquez;Lilián Yépez;A. Hernández-Campos;A. Tapia;F. Hernández‐Luis;R. Cedillo;
阿苯达唑 (Abz) 和甲苯达唑 (Mbz) 类似物已被合成，并在体外针对原生动物兰氏贾第鞭毛虫、阴道毛滴虫以及蠕虫旋毛虫和秀丽隐杆线虫进行了测试。结果表明，化合物 4a、4b（Abz 类似物）、12b 和 20（Mbz 类似物）与甲硝唑一样具有抗原虫活性。化合物 9 对抗阴道毛滴虫的活性比 Abz 高 58 倍。化合物 8 和 4a 也显示出针对这种原生动物的高活性。化合物 4b 和 5a 的活性与 Abz 一样。甲苯咪唑类似物均未表现出抗阴道毛滴虫的活性。这些化合物的驱虫活性很差。
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.