取代查耳酮的溶液相平行合成及其对蓝氏贾第鞭毛虫的抗寄生虫活性。
Solution-phase parallel synthesis of substituted chalcones and their antiparasitary activity against Giardia lamblia.
作者信息
Montes-Avila Julio, Díaz-Camacho Sylvia P, Sicairos-Félix Josefina, Delgado-Vargas Francisco, Rivero I A
机构信息
Centro de Graduados e Investigación, Instituto Tecnológico de Tijuana, PO Box 1166, 22000 Tijuana, B.C., Mexico.
出版信息
Bioorg Med Chem. 2009 Sep 15;17(18):6780-5. doi: 10.1016/j.bmc.2009.02.052. Epub 2009 Mar 3.
A library of 25-membered chalcones was prepared by parallel synthesis. Substituted acetophenones and benzaldehydes were condensed using the Claisen-Schmidt base-catalyzed aldol condensation. Several chalcones showed in vitro antiparasitic activity against Giardia lamblia. The highest activity observed for the IC(50) values were 12.72, 15.05 and 15.31 microg/mL, respectively; these are potential leads for the development of antigiardial compounds.
通过平行合成制备了一个包含25元查耳酮的文库。使用克莱森-施密特碱催化的羟醛缩合反应使取代苯乙酮和苯甲醛缩合。几种查耳酮对蓝氏贾第鞭毛虫显示出体外抗寄生虫活性。观察到的IC(50)值的最高活性分别为12.72、15.05和15.31微克/毫升；这些是开发抗贾第虫化合物的潜在先导物。
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