Achiral, cheap, and potent inhibitors of plasmepsins I, II, and IV

被引：47

作者：

Boss, Christoph

Corminboeuf, Olivier

Grisostomi, Corinna

Meyer, Solange

Jones, Andrew F.

Prade, Lars

Binkert, Christoph

Fischli, Walter

Weller, Thomas

Bur, Daniel

机构：

[1] Drug Discovery, Chemistry and Biology, Actelion Pharmaceuticals Ltd., 4123 Allschwil

来源：

CHEMMEDCHEM | 2006年 / 1卷 / 12期

关键词：

Aspartic proteases; Drug design; Inhibitors; Malaria; Medicinal chemistry;

D O I：

10.1002/cmdc.200600223

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel class of molecules targeting aspartic proteinases from P falciparum is described. Synthesis of these easily available, achiral, and highly potent molecules was supported by structural information and eventually allowed the identification of compounds highly active against three vacuolar aspartic proteinases. In a red blood cell assay, the growth of P. falciparurn (strain K1) could be effectively prevented.

引用

收藏

页码：1341 / +

页数：6

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