Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 9, Pages 2606-2610Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.01.101
Keywords
Berberine; 5,6-Didehydro-8,8-diethyl-13-oxodihydroberberine chloride; African trypanosomiasis; Leishmaniasis; Malaria; Inhibitory activity
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Funding
- College of Pharmacy, The Ohio State University
- Bill and Melinda Gates Foundation
- NSF [CHE-0130903]
- Galician Conselleria de Educacion [2009/071]
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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.
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