Starving the malaria parasite:: Inhibitors active against the aspartic proteases plasmepsins I, II, and IV

被引：76

作者：

Hof, F

Schütz, A

Fäh, C

Meyer, S

Bur, D

Liu, J

Goldberg, DE

Diederich, F

机构：

[1] ETH, Organ Chem Lab, HCI, CH-8093 Zurich, Switzerland

[2] Univ Victoria, Dept Chem, STN CSC, Victoria, BC V8W 3V6, Canada

[3] Actel Pharmaceut, CH-4123 Allschwil, Switzerland

[4] Washington Univ, Howard Hughes Med Inst, Dept Med, St Louis, MO 63110 USA

[5] Washington Univ, Howard Hughes Med Inst, Dept Mol Microbiol, St Louis, MO 63110 USA

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2006年 / 45卷 / 13期

关键词：

aspartic proteases; drug design; inhibitors; malaria; medicinal chemistry;

D O I：

10.1002/anie.200504119

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Clamping down: A new class of aspartic protease inhibitors that target the malarial protease family Plasmepsin are reported. These ligands utilize a novel "diamine clamp" to engage the catalytic dyad. They are potent inhibitors of plasmepsins I, II, and IV, while retaining good selectivity against the closely related human cathepsins D and E. (Chemical Equation Presented) .© 2006 Wiley-VCH Verlag GmbH & Co. KGaA.

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页码：2138 / 2141

页数：4

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