1241906-93-3Relevant academic research and scientific papers
1-Azaaurones derived from the naturally occurring aurones as potential antimalarial drugs
Souard, Florence,Okombi, Sabrina,Beney, Chantal,Chevalley, Severine,Valentin, Alexis,Boumendjel, Ahcne
scheme or table, p. 5724 - 5731 (2010/09/09)
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.
