二咪唑啉酰胺对非洲锥虫病的活性。
Activity of diimidazoline amides against African trypanosomiasis.
作者信息
Dong Yuxiang, Wang Xiaofang, Cal Monica, Kaiser Marcel, Vennerstrom Jonathan L
机构信息
College of Pharmacy, University of Nebraska Medical Center, 986025 Nebraska Medical Center, Omaha, NE, USA.
Swiss Tropical and Public Health Institute, Socinstrasse 57, CH-4002 Basel, Switzerland; University of Basel, CH-4003 Basel, Switzerland.
出版信息
Bioorg Med Chem Lett. 2014 Feb 1;24(3):944-8. doi: 10.1016/j.bmcl.2013.12.064. Epub 2013 Dec 22.
Abstract
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.
摘要
我们鉴定出了几种二咪唑啉单酰胺和二酰胺，它们在体外对布氏罗得西亚锥虫的活性与喷他脒相当。所有这些化合物的细胞毒性也都比喷他脒小，但在布氏罗得西亚锥虫感染的小鼠模型中，没有一种化合物的效果能与后者相媲美。只要存在第二个弱碱官能团，单个咪唑啉可能就足以产生高抗锥虫活性。
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