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
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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