Activity of diimidazoline amides against African trypanosomiasis

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• 作者：Yuxiang Dong ; Xiaofang Wang ; Monica Cal ; Marcel Kaiser ; Jonathan L. Vennerstrom
• 关键词：Diimidazoline ; African trypanosomiasis ; Trypanosoma brucei rhodesiense
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：1 February, 2014
• 年：2014
• 卷：24
• 期：3
• 页码：944-948
• 全文大小：685 K

文摘

We identified several diimidazoline mono- and diamides that were as potent as pentamidine against Trypanosoma brucei rhodesiense in vitro. All of these were also less cytotoxic than pentamidine, but none was as effective as the latter in a T. brucei rhodesiense-infected mouse model. A single imidazoline may be sufficient for high antitrypanosomal activity provided that a second weak base functional group is present.