2-CARBOXY INDOLINES AND INDOLES AS POTENTIAL GLYCINE/NMDA ANTAGONISTS - EFFECT OF 5-MEMBERED RING CONFORMATION ON AFFINITY

被引：16

作者：

ROWLEY, M

LEESON, PD

GRIMWOOD, S

FOSTER, A

SAYWELL, K

机构：

[1] Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex CM20 2QR, Terlings Park, Eastwick Road

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1992年 / 2卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(00)80444-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

2-Carboxy indolines were synthesised as potential antagonists at the glycine site of the NMDA receptor, based on a pharmacophore developed from other series. None of the indolines had significant potency, possibly due to the lack of coplanarity of the carboxyl with the aromatic ring. The corresponding indoles are potent antagonists, as exemplified by 19, IC50 27 nM.

引用

页码：1627 / 1630

页数：4

共 7 条

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