Mar 2010 European journal of medicinal chemistry

Synthesis and antiprotozoal activity of 4-arylcoumarins.

Auteurs

Pierson JT, Dumètre A, Hutter S, Delmas F, Laget M, Finet JP, Azas N, Combes S

Résumé

A large series of 4-arylcoumarins was synthesized by Suzuki-Miyaura cross-coupling reaction and evaluated for antiprotozoal activity against Plasmodium falciparum and Leishmania donovani. Several compounds were found to strongly inhibit the proliferation of human cell line and/or parasites. The 4-(3,4-dimethoxyphenyl)-6,7-dimethoxycoumarin exhibit a potent activity on L. donovani amastigotes with a selectivity index (SI=265) twice than amphotericin B (SI=140).

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