期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 9, 页码 2606-2610出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.01.101
关键词
Berberine; 5,6-Didehydro-8,8-diethyl-13-oxodihydroberberine chloride; African trypanosomiasis; Leishmaniasis; Malaria; Inhibitory activity
资金
- College of Pharmacy, The Ohio State University
- Bill and Melinda Gates Foundation
- NSF [CHE-0130903]
- Galician Conselleria de Educacion [2009/071]
Treatment of diseases such as African sleeping sickness and leishmaniasis often depends on relatively expensive or toxic drugs, and resistance to current chemotherapeutics is an issue in treating these diseases and malaria. In this study, a new semi-synthetic berberine analogue, 5,6-didehydro-8, 8-diethyl-13-oxodihydroberberine chloride (1), showed nanomolar level potency against in vitro models of leishmaniasis, malaria, and trypanosomiasis as well as activity in an in vivo visceral leishmaniasis model. Since the synthetic starting material, berberine hemisulfate, is inexpensive, 8,8-dialkyl-substituted analogues of berberine may lead to a new class of affordable antiprotozoal compounds. (C) 2011 Published by Elsevier Ltd.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据