DESIGN, SYNTHESIS AND MOLECULAR MODELING OF 3-ACYLAMINO-2-CARBOXYINDOLE NMDA RECEPTOR GLYCINE-SITE ANTAGONISTS

被引：26

作者：

SALITURO, FG

TOMLINSON, RC

BARON, BM

DEMETER, DA

WEINTRAUB, HJR

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)81105-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The syntheses and molecular modeling of several 3-acylamino-2-carboxyindole antagonists of the glycine binding site associated with the NMDA receptor complex is described. Tertiary amide 8 is a potent antagonist; this result is rationalized by a preferred cis amide bond conformation. The potency of the trans secondary oxalamide 10 is explained by binding to the receptor in its enolic form.

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页码：455 / 460

页数：6

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