The synthesis of β-strand mimetic templates via regioselective 1,3-dipolar cycloaddition with vinylsulfone

被引:26
|
作者
Fuchi, N
Doi, T
Harada, T
Urban, J
Cao, BL
Kahn, M
Takahashi, T
机构
[1] Tokyo Inst Technol, Grad Sch Sci & Engn, Dept Appl Chem, Tokyo 1528552, Japan
[2] Molecumet Ltd, Bellevue, WA 98005 USA
[3] Univ Washington, Dept Pathobiol, Seattle, WA 98195 USA
关键词
1,3-dipolar cycloaddition; vinyl sulfone; peptidomimetics; serine protease inhibitor;
D O I
10.1016/S0040-4039(00)02229-2
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
We have developed a practical synthetic route to constrained P-strand mimetic templates by regioselective 1,3-dipolar cycloaddition of azomethine imines with vinyl sulfone. A small library of P-strand mimetic templates was generated which include potent and selective inhibitors of serine proteases. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1305 / 1308
页数:4
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