Novel N1-(benzyl)cinnamamidine derived NR2B subtype-selective NMDA receptor antagonists

被引：30

作者：

Curtis, NR

Diggle, HJ

Kulagowski, JJ

London, C

Grimwood, S

Hutson, PH

Murray, F

Richards, P

Macaulay, A

Wafford, KA

机构：

[1] Merck Sharp & Dohme Res Labs, Dept Med Chem, Ctr Res Neurosci, Harlow CM20 2QR, Essex, England

[2] Merck Sharp & Dohme Res Labs, Dept Behav Neurosci, Ctr Res Neurosci, Harlow CM20 2QR, Essex, England

[3] Merck Sharp & Dohme Res Labs, Dept Pharmacol, Ctr Res Neurosci, Harlow CM20 2QR, Essex, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 04期

关键词：

D O I：

10.1016/S0960-894X(02)01060-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Novel (E)-N-1-(benzyl)cinnamamidines were prepared and evaluated as NR2B subtype NMDA receptor ligands. Excellent affinity was achieved by appropriate substitution of either phenyl ring. The 2-methoxybenzyl compound 1h had similar to1000-fold lower IC50 in NR2B than NR2A-containing cells. Replacement of the styryl unit by 2-naphthl was well tolerated. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：693 / 696

页数：4

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