1,2,4-Trioxanes as potential antimalarial agents
- 1 April 1988
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 31 (4) , 713-716
- https://doi.org/10.1021/jm00399a004
Abstract
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-epidoxy-4a,5,6,7,8,8a-hexahydro-5,5,8a-trimethyl-2H-1-benzopyran-2-yl)acetate (3b), which showed IC50''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]-5,5,8a-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.This publication has 3 references indexed in Scilit:
- Endoperoxides as potential antimalarial agentsJournal of Medicinal Chemistry, 1987
- In vitro activities of and mechanisms of resistance to antifol antimalarial drugsAntimicrobial Agents and Chemotherapy, 1985
- 2,4,7-Triamino-6-ortho-substituted Arylpteridines. A New Series of Potent Antimalarial AgentsJournal of Medicinal Chemistry, 1967