Synthesis and antiprotozoal activity of 4-arylcoumarins

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).

Synthesis and biological evaluation of 4-arylcoumarins as antiprotozoal agents were investigated. The 4-(3,4-dimethoxyphenyl)-6,7-dimethoxycoumarin was found to exhibit a potent activity on Leishmania donovani amastigotes with a selectivity index (SI = 265) twice than amphotericin B (SI = 140).Figure optionsDownload as PowerPoint slide