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1-[5-(5-硝基呋喃-2-基)-1,3,4-噻二唑-2-基]-和1-[5-(5-硝基噻吩-2-基)-1,3,4-噻二唑-2-基]-4-芳酰基哌嗪的合成及其体外抗利什曼原虫活性

Synthesis and in vitro anti-leishmanial activity of 1-[5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2-yl]- and 1-[5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-yl]-4-aroylpiperazines.

作者信息

Behrouzi-Fardmoghadam Mina, Poorrajab Fatemeh, Ardestani Sussan Kaboudanian, Emami Saeed, Shafiee Abbas, Foroumadi Alireza

机构信息

Department of Medicinal Chemistry, Faculty of Pharmacy & Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran 14174, Iran.

出版信息

Bioorg Med Chem. 2008 Apr 15;16(8):4509-15. doi: 10.1016/j.bmc.2008.02.052. Epub 2008 Feb 20.

Abstract

The synthesis and anti-leishmanial activity of nitroheteroaryl-1,3,4-thiadiazole-based compounds including 1-[5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2-yl]-4-aroylpiperazines and 1-[5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-yl]-4-aroylpiperazines were described. Most of the synthesized compounds exhibited potent anti-leishmanial activity against both promastigote and amastigote forms of Leishmania major at non-cytotoxic concentrations. In general, 5-nitrofuran derivatives were more active than the corresponding 5-nitrothiophene analogues.

摘要

含1-[5-(5-硝基呋喃-2-基)-1,3,4-噻二唑-2-基]-4-芳酰基哌嗪和1-[5-(5-硝基噻吩-2-基)-1,3,4-噻二唑-2-基]-4-芳酰基哌嗪的基于硝基杂芳基-1,3,4-噻二唑的化合物的合成及其抗利什曼原虫活性已被描述。大多数合成化合物在无细胞毒性浓度下对硕大利什曼原虫的前鞭毛体和无鞭毛体形式均表现出强效抗利什曼原虫活性。一般来说,5-硝基呋喃衍生物比相应的5-硝基噻吩类似物更具活性。

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