From peptides to non-peptide peptidomimetics: Design and synthesis of new piperidine inhibitors of aspartic peptidases

被引：58

作者：

Bursavich, MG

West, CW

Rich, DH

机构：

[1] Univ Wisconsin, Dept Chem, Madison, WI 53706 USA

[2] Univ Wisconsin, Sch Pharm, Madison, WI 53705 USA

来源：

ORGANIC LETTERS | 2001年 / 3卷 / 15期

关键词：

D O I：

10.1021/ol016092u

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

[GRAPHICS] The 3-alkoxy-4-arylpiperidine inhibitors of aspartic peptidases are shown to be a new type of non-peptide peptidomimetic inhibitor. These piperidines can be designed from peptide derived inhibitors by use of a structure generating program but only after the enzyme active site conformation has been modified in a mechanistically related fashion. New enantioselective syntheses of 3-alkoxy-4-arylpiperidine analogues are described.

引用

页码：2317 / 2320

页数：4

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