Synthesis of macrocyclic trypanosomal cysteine protease inhibitors

被引：37

作者：

Chen, Yen Ting ^{[1
,2
]}

Lira, Ricardo ^{[1
,2
]}

Hansell, Elizabeth ^{[3
]}

McKerrow, James H. ^{[3
]}

Roush, William R. ^{[1
,2
]}

机构：

[1] Scripps Florida, Dept Chem, Jupiter, FL 33458 USA

[2] Univ Michigan, Dept Chem, Ann Arbor, MI 48109 USA

[3] Univ Calif San Francisco, Sander Ctr Basic Res Parasit Dis, San Francisco, CA 94143 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 22期

关键词：

Cysteine protease inhibitors; Macrocyclic dipeptidyl vinyl sulfones;

D O I：

10.1016/j.bmcl.2008.06.012

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The importance of cysteine proteases in parasites, compounded with the lack of redundancy compared to their mammalian hosts makes proteases attractive targets for the development of new therapeutic agents. The binding mode of K11002 to cruzain, the major cysteine protease of Trypanosoma cruzi was used in the design of conformationally constrained inhibitors. Vinyl sulfone-containing macrocycles were synthesized via olefin ring-closing metathesis and evaluated against cruzain and the closely related cysteine protease, rhodesain. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：5860 / 5863

页数：4

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