SYNTHESIS OF 3(S)-PHOSPHONOACETYL-2(R)-PIPERIDINECARBOXYLIC ACID - A CONFORMATIONALLY-RESTRICTED GLUTAMATE ANTAGONIST

被引：29

作者：

WHITTEN, JP

MUENCH, D

CUBE, RV

NYCE, PL

BARON, BM

MCDONALD, IA

机构：

[1] Marion Merrell Dow Research Institute, Cincinnati, OH 45215

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1991年 / 1卷 / 09期

关键词：

D O I：

10.1016/S0960-894X(01)81102-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of the conformationally-restricted beta-ketophosphonic acid, 3(S)-phosphonoacetyl-2(R)-piperidinecarboxylic acid (4) is described. This compound is a competitive, glutamate antagonist (IC50 = 40 nM vs [H-3]CPP) of the NMDA receptor complex.

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页码：441 / 444

页数：4

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