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ChemInform Abstract: New Type of Febrifugine Analogues, Bearing a Quinolizidine Moiety, Show Potent Antimalarial Activity Against Plasmodium Malaria Parasite
- Source :
- ChemInform. 30
- Publication Year :
- 2010
- Publisher :
- Wiley, 2010.
-
Abstract
- Febrifugine (1) and isofebrifugine (2), isolated from the roots of Dichroa febrifuga Lour. (Chinese name: Chang Shan), are active principles against malaria. Adducts of 1 and 2 with acetone, Df-1 (3) and Df-2 (4), respectively, were obtained using silica gel and acetone. They showed high activity against P. falciparum malaria in vitro. Compound 3 was found to be equally effective against P. berghei in vivo as the clinically used drug chloroquine, whereas 4 showed only 1/24 of the activity of 3. Metabolism studies of these compounds revealed that compound 4 is readily metabolized in mouse liver. Accordingly, the dose of 4 must be higher than that of 3 to attain blood levels sufficient for a favorable therapeutic effect.
Details
- ISSN :
- 15222667 and 09317597
- Volume :
- 30
- Database :
- OpenAIRE
- Journal :
- ChemInform
- Accession number :
- edsair.doi...........61b9d808fda30d19d88b5bbb4ade4996