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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and in vitro trichomonicidal, giardicidal and amebicidal activity of N-acetamide(sulfonamide)-2-methyl-4-nitro-1H-imidazoles.
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Synthesis and in vitro trichomonicidal, giardicidal and amebicidal activity of N-acetamide(sulfonamide)-2-methyl-4-nitro-1H-imidazoles.

机译：N-乙酰胺（磺酰胺）-2-甲基-4-硝基-1H-咪唑的合成及体外杀螨，杀螨和杀螨活性。

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摘要

Two new series of imidazole derivatives (acetamides: 1-8 and sulfonamides: 9-15) were synthesized using a short synthetic route. Compound 1 as well as the intermediate 16g were characterized by X-ray crystallography. Imidazole derivatives 1-15 were tested in vitro against three unicellular parasites (Giardia intestinalis, Trichomonas vaginalis and Entamoeba histolytica) in comparison with benznidazole (Bzn) and metronidazole. Compound 1 [N-benzyl-2-(2-methyl-4-nitro-1H-imidazol-1-yl)acetamide] was 2 times more active than Bzn against T. vaginalis and G. intestinalis and it was as active as Bzn against E. histolytica. Sulfonamides showed selective toxicity against E. histolytica over the other parasites. Toxicity assay showed that all compounds are non-cytotoxic against MDCK cell line. The results revealed that compounds 1-15 have antiparasitic bioactivity in the micromolar range against the parasites tested, and could be considered as benznidazole bioisosteres.
机译：使用短合成路线合成了两个新系列的咪唑衍生物（乙酰胺：1-8和磺酰胺：9-15）。通过X射线晶体学表征化合物1以及中间体16g。与苯并硝唑（Bzn）和甲硝唑相比，咪唑衍生物1-15在体外针对三种单细胞寄生虫（肠道贾第鞭毛虫，阴道毛滴虫和组织变形杆菌）进行了测试。化合物1 [N-苄基-2-（2-甲基-4-硝基-1H-咪唑-1-基）乙酰胺]对B.n.阴道曲霉和肠道小肠念珠菌的活性是Bzn的2倍，并且活性与Bzn相同对抗溶组织性大肠杆菌。磺胺类药物对其他组织寄生虫表现出针对组织溶大肠杆菌的选择性毒性。毒性试验表明，所有化合物均对MDCK细胞系无细胞毒性。结果表明，化合物1-15在微摩尔范围内对测试的寄生虫具有抗寄生生物活性，可以被视为苯并硝唑生物等排体。

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