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[具有抗寄生虫活性的新型咪唑二杂环衍生物的合成]

[Synthesis of new diheterocyclic derivatives of imidazole with antiparasitic activity].

作者信息

Quattara L, Debaert M, Cavier R

出版信息

Farmaco Sci. 1987 May;42(5):383-96. doi: 10.1002/chin.198748101.

DOI:10.1002/chin.198748101
PMID:2886364
Abstract

A description is given of potential cyclic imidazoles such as 3,3-dichloro-2-methylenimino-acrylonitrile derived from nitro or non-nitro heterocycles, as well as the hydrazone, semicarbazone and arylpropenone derivatives of the 4-chloro-2-(5-nitro-2-thienyl) (V), 5-imidazole carboxaldehyde (IV) and the 5-bromothienyl analogue. The antiparasitic activity was tested in vitro against Trichomonas vaginalis and Entameba histolytica. Some of the nitro containing compounds showed trichomonacidal activity whereas one of the non-nitro compounds with potential imidazole structure showed clear amebacidal activity. This compound, 3,3-dichloro-2-methyleneimino acrylonitrile has anti-ameba activity comparable with that of metronidazole.

摘要

描述了由硝基或非硝基杂环衍生的潜在环状咪唑,如3,3-二氯-2-亚甲基亚氨基丙烯腈,以及4-氯-2-(5-硝基-2-噻吩基)(V)、5-咪唑甲醛(IV)和5-溴噻吩类似物的腙、氨基脲和芳基丙烯酮衍生物。对阴道毛滴虫和溶组织内阿米巴进行了体外抗寄生虫活性测试。一些含硝基的化合物表现出杀滴虫活性,而一种具有潜在咪唑结构的非硝基化合物表现出明显的杀阿米巴活性。这种化合物,3,3-二氯-2-亚甲基亚氨基丙烯腈具有与甲硝唑相当的抗阿米巴活性。

相似文献

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[Synthesis of new diheterocyclic derivatives of imidazole with antiparasitic activity].[具有抗寄生虫活性的新型咪唑二杂环衍生物的合成]
Farmaco Sci. 1987 May;42(5):383-96. doi: 10.1002/chin.198748101.
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Antiparasitic nitroimidazoles. 1. Some 2-styryl-5-nitroimidazoles.抗寄生虫硝基咪唑类。1. 一些2-苯乙烯基-5-硝基咪唑类。
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[Synthesis and antiparasitic activity of new nitro-5-imidazole derivatives].新型硝基-5-咪唑衍生物的合成及其抗寄生虫活性
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Biochem Pharmacol. 1973 Mar 1;22(5):639-49. doi: 10.1016/0006-2952(73)90378-x.

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