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1-Azaaurones derived from the naturally occurring aurones as potential antimalarial drugs.

par Souard, Florence ;Okombi, Sabrina;Beney, Chantal;Chevalley-Maurel, Séverine;Valentin, Alexis;Boumendjel, Ahcène
Référence Bioorganic & medicinal chemistry, 18, 15, page (5724-5731)
Publication Publié, 2010-08

Article révisé par les pairs

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Résumé :

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.