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
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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