1,2,4-Trioxanes as potential antimalarial agents.
Journal Article (Journal Article)
A number of 1,2,4-trioxanes were prepared and tested for antimalarial activity in search of a simplified analogue of the naturally occurring antimalarial qinghaosu. The compounds were assayed in an in vitro system for antimalarial activity against chloroquine-susceptible and chloroquine-resistant strains of Plasmodium falciparum. The most active compounds were methyl 2-(2,4a-epidioxy-4a,5,6,7,8,8a-hexahydro-5,5,8a-trimethyl-2H-1-benzop yra n-2-yl) acetate (3b), which showed IC20's of 96 and 39 ng/mL, respectively, and 2,4a-epidioxy-3,4,4a,5,6,7,8,8a-octahydro-2-[2-(benzoyloxy)propyl]-5,5,8 a- trimethyl-2H-1-benzopyran (12), which showed IC50's of 24 and 99 ng/mL, respectively. For comparison, qinghaosu exhibits an IC50 of 1 ng/mL for both strains.
Full Text
Duke Authors
Cited Authors
- Kepler, JA; Philip, A; Lee, YW; Morey, MC; Carroll, FI
Published Date
- April 1, 1988
Published In
Volume / Issue
- 31 / 4
Start / End Page
- 713 - 716
PubMed ID
- 3280797
International Standard Serial Number (ISSN)
- 0022-2623
Digital Object Identifier (DOI)
- 10.1021/jm00399a004
Language
- eng
Conference Location
- United States