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基于色烯的合成查耳酮类化合物作为有效的抗利什曼原虫药物:合成与生物活性。

Chromene-based synthetic chalcones as potent antileishmanial agents: synthesis and biological activity.

机构信息

Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran 14174, Iran.

出版信息

Chem Biol Drug Des. 2010 Jun;75(6):590-6. doi: 10.1111/j.1747-0285.2010.00959.x. Epub 2010 Mar 10.

Abstract

Two types of regioisomeric chromene-based chalcones namely, 1-(6-methoxy-2H-chromen-3-yl)-3-phenylpropen-1-ones and 3-(6-methoxy-2H-chromen-3-yl)-1-phenylpropen-1-ones were prepared and investigated for their antileishmanial activity against promastigotes form of Leishmania major. The obtained results from in vitro biological assays indicated that chloro-substituted 1-(6-methoxy-2H-chromen-3-yl)-3-phenylpropen-1-ones exhibited excellent activity against Leishmania major at non-cytotoxic concentrations.

摘要

两种类型的区域异构色烯查尔酮,即 1-(6-甲氧基-2H-色烯-3-基)-3-苯基丙烯-1-酮和 3-(6-甲氧基-2H-色烯-3-基)-1-苯基丙烯-1-酮被制备并研究了它们对利什曼原虫的抗利什曼原虫活性。体外生物测定结果表明,氯取代的 1-(6-甲氧基-2H-色烯-3-基)-3-苯基丙烯-1-酮在非细胞毒性浓度下对利什曼原虫表现出优异的活性。

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