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.
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页码：693 / 696
页数：4
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