Tryptanthrin derivatives as Toxoplasma gondii inhibitors-structure-activity-relationship of the 6-position

被引：51
作者：
Krivogorsky, Bogdana [1 ]
Nelson, Amber C. [1 ]
Douglas, Kelsi A. [1 ]
Grundt, Peter [1 ]
机构：
[1] Univ Minnesota, Dept Chem & Biochem, Duluth, MN 55812 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 04期
关键词：
Toxoplasma gondii; Tryptanthrin; Inhibition of parasite growth; Natural product; IN-VITRO; CONGENITAL TOXOPLASMOSIS; UNITED-STATES; INFECTION; ANALOGS; ARTEMISININ;
D O I：
10.1016/j.bmcl.2012.12.024
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A panel of derivatives of the natural product tryptanthrin was synthesized and screened for its in vitro activity against the intracellular parasite Toxoplasma gondii. We concentrated on the modification of the 6-keto group of tryptanthrin and prepared a series of oximes, hydrazones and alcohols based on tryptanthrin. We evaluated parasite growth inhibition and host cell cytotoxicity. Our results indicate that in particular alcohol analogs are promising candidates for further investigation. (C) 2012 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1032 / 1035
页数：4
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