4-芳基香豆素的合成及抗原虫活性。
Synthesis and antiprotozoal activity of 4-arylcoumarins.
机构信息
Faculté des Sciences de Saint-Jérôme, UMR-CNRS 6264, Laboratoire Chimie Provence, Universités Aix-Marseille I, II and III, 13397 Marseille Cedex 20, France.
出版信息
Eur J Med Chem. 2010 Mar;45(3):864-9. doi: 10.1016/j.ejmech.2009.10.022. Epub 2009 Oct 23.
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).
通过 Suzuki-Miyaura 交叉偶联反应合成了一系列 4-芳基香豆素，并对其抗疟原虫和利什曼原虫的活性进行了评估。发现一些化合物强烈抑制人细胞系和/或寄生虫的增殖。4-(3,4-二甲氧基苯基)-6,7-二甲氧基香豆素对利什曼原虫无鞭毛体具有很强的活性，其选择性指数（SI=265）是两性霉素 B（SI=140）的两倍。
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