1. Synthesis and antimalarial activity of new atovaquone derivatives.
- Author
-
El Hage S, Ane M, Stigliani JL, Marjorie M, Vial H, Baziard-Mouysset G, and Payard M
- Subjects
- Antimalarials chemical synthesis, Atovaquone chemical synthesis, Parasitic Sensitivity Tests, Structure-Activity Relationship, Antimalarials chemistry, Antimalarials pharmacology, Atovaquone analogs & derivatives, Atovaquone pharmacology, Malaria, Falciparum drug therapy, Plasmodium falciparum drug effects
- Abstract
In this paper we describe the design and synthesis of 18 derivatives of the antimicrobial atovaquone which were substituted at the 3-hydroxy group by ester and ether functions. The compounds were evaluated in vitro for their activity against the growth of Plasmodium falciparum, the malaria causing parasite. All the compounds showed potent activity, with IC(50) values in the range of 1.25-50 nM, comparable to those of atovaquone and much higher than chloroquine or quinine. more...
- Published
- 2009
- Full Text
- View/download PDF