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Potent antiprotozoal activity of a novel semi-synthetic berberine derivative.

Abstract：

: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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Bahar M,Deng Y,Zhu X,He S,Pandharkar T,Drew ME,Navarro-Vázquez A,Anklin C,Gil RR,Doskotch RW,Werbovetz KA,Kinghorn AD

doi

10.1016/j.bmcl.2011.01.101

subject

Has Abstract

pub_date

2011-05-01 00:00:00

pages

2606-10

issue

9

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)00124-7

journal_volume

21

pub_type

杂志文章

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