Activity of amidine-containing diphenylureas against P-falciparum

被引：5

作者：

Bhattacharya, G

Gerena, L

Jiang, SP

Werbovetz, KA

机构：

[1] Ohio State Univ, Coll Pharm, Div Med Chem & Pharmacognosy, Columbus, OH 43210 USA

[2] Walter Reed Army Inst Res, Div Expt Therapeut, Silver Spring, MD 20910 USA

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2005年 / 2卷 / 02期

关键词：

diamidine; antimalarial; Plasmodium falciparum; plasmepsin; heme assembly;

D O I：

10.2174/1570180053175061

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Amidine-containing derivatives of the diphenylurea antimalarial lead compound WR268961, a putative plasmepsin inhibitor, were prepared and tested against erythtocyte-stage P. falciparum. Diamidine 8 was the most active compound, displaying IC50 Values of 54 nM and 41 nM versus chloroquine sensitive (D6) and chloroquine resistant (W2) parasites, respectively.

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收藏

页码：162 / 164

页数：3

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