Potent antiprotozoal activity of a novel semi-synthetic berberine derivative.
Bioorg Med Chem Lett
; 21(9): 2606-10, 2011 May 01.
Article
in En
| MEDLINE
| ID: mdl-21474310
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.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Parasites
/
Protozoan Infections
/
Berberine
/
Antiprotozoal Agents
Limits:
Animals
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2011
Document type:
Article
Affiliation country:
United States