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1-Azaaurones derived from the naturally occurring aurones as potential antimalarial drugs.
Souard, Florence; Okombi, Sabrina; Beney, Chantal; Chevalley, Séverine; Valentin, Alexis; Boumendjel, Ahcène.
Afiliação
  • Souard F; Département 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
Bioorg Med Chem ; 18(15): 5724-31, 2010 Aug 01.
Article em En | MEDLINE | ID: mdl-20630767
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.
Assuntos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Compostos Aza / Benzofuranos / Indóis / Antimaláricos Limite: Humans Idioma: En Ano de publicação: 2010 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Compostos Aza / Benzofuranos / Indóis / Antimaláricos Limite: Humans Idioma: En Ano de publicação: 2010 Tipo de documento: Article