Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, Cuernavaca, Morelos 62209, Mexico.
Bioorg Med Chem. 2010 Sep 1;18(17):6398-403. doi: 10.1016/j.bmc.2010.07.008. Epub 2010 Jul 30.
We have synthesized a new series of quinoline tripartite hybrids from chloroquine, ethambutol, and isoxyl drugs, using a short synthetic route. Compounds 1-8 were tested in vitro against five protozoa (Giardia intestinalis, Trichomonas vaginalis,Entamoeba histolytica, Leishmania mexicana and Trypanosoma cruzi) and Mycobacterium tuberculosis. N-(4-Butoxyphenyl)-N'-{2-[(7-chloroquinolin-4-yl)amino]ethyl}urea (6) was the most active compound against all parasites tested. Compound 6 was 670 times more active than metronidazole, against G. intestinalis. It was as active as pentamidine against L. mexicana, and it was twofold more potent than ethambutol and isoxyl versus M. tuberculosis. This compound could be considered as a new broad spectrum antimicrobial agent.
我们从氯喹、乙胺丁醇和异羟肟酸药物合成了一系列新的喹啉三联体杂种，采用了短的合成路线。将化合物 1-8 进行了体外测试，对抗五种原生动物（肠道贾第鞭毛虫、阴道毛滴虫、溶组织内阿米巴、墨西哥利什曼原虫和克氏锥虫）和结核分枝杆菌。N-(4-丁氧基苯基）-N'-{2-[(7-氯喹啉-4-基）氨基]乙基}脲（6）是对抗所有测试寄生虫最有效的化合物。化合物 6 对 G. intestinalis 的活性比甲硝唑高 670 倍。它对 L. mexicana 的活性与戊烷脒相当，对 M. tuberculosis 的活性比乙胺丁醇和异羟肟酸强两倍。该化合物可被视为一种新的广谱抗菌剂。
