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1-Azaaurones derived from the naturally occurring aurones as potential antimalarial drugs
Florence Souard1, Sabrina Okombi, Chantal Beney
1Département de Pharmacochimie Moléculaire, Université de Grenoble I/CNRS, UMR 5063, 470 rue de la Chimie, BP 53 F-38041, Grenoble Cedex 9, France. florence.souard@ujf-grenoble.fr
Abstract:
We report the synthesis and in vitro antiplasmodial activity of 35 compounds, designed as analogues of the naturally occurring aurones. Several of these analogues showed submicromolar antimalarial activity against a chloroquine-resistant strain of Plasmodium falciparum (FcB1-Columbia strain) cultured on human erythrocytes. Substitution of the intracyclic oxygen in aurones by a nitrogen atom and systematic variation of the substituent at the B-ring revealed promising leads showing good activity on the CQ-resistant strain. In particular, 4,6-dimethoxy-4'-ethylazaaurone 22 showed antiplasmodial potency without noticeable toxicity. The easy synthesis of this family of compounds and the relevant antiplasmodial activity are in favor of promising candidates for further development.
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