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

Neil R. Curtis; Helen J. Diggle; Janusz J. Kulagowski; Clare London; Sarah Grimwood; Peter H. Hutson; Fraser Murray; Pawel Richards; Alison Macaulay; Keith A. Wafford

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

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

Neil R. Curtis, Helen J. Diggle, Janusz J. Kulagowski, Clare London, Sarah Grimwood, Peter H. Hutson, Fraser Murray, Pawel Richards, Alison Macaulay, Keith A. Wafford

Research output: Contribution to journal › Article › peer-review

Abstract

Novel (E)-N1-(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 ∼1000-fold lower IC50 in NR2B than NR2A-containing cells. Replacement of the styryl unit by 2-naphthyl was well tolerated. © 2003 Elsevier Science Ltd. All rights reserved.

Original language	English
Pages (from-to)	693-696
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	13
Issue number	4
DOIs	https://doi.org/10.1016/S0960-894X(02)01060-0
Publication status	Published - Feb 2003

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

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title = "Novel N1-(benzyl)cinnamamidine derived NR2B subtype-selective NMDA receptor antagonists",

abstract = "Novel (E)-N1-(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 ∼1000-fold lower IC50 in NR2B than NR2A-containing cells. Replacement of the styryl unit by 2-naphthyl was well tolerated. {\textcopyright} 2003 Elsevier Science Ltd. All rights reserved.",

author = "Curtis, {Neil R.} and Diggle, {Helen J.} and Kulagowski, {Janusz J.} and Clare London and Sarah Grimwood and Hutson, {Peter H.} and Fraser Murray and Pawel Richards and Alison Macaulay and Wafford, {Keith A.}",

year = "2003",

month = feb,

doi = "10.1016/S0960-894X(02)01060-0",

language = "English",

volume = "13",

pages = "693--696",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "1464-3405",

publisher = "Elsevier BV",

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TY - JOUR

T1 - Novel N1-(benzyl)cinnamamidine derived NR2B subtype-selective NMDA receptor antagonists

AU - Curtis, Neil R.

AU - Diggle, Helen J.

AU - Kulagowski, Janusz J.

AU - London, Clare

AU - Grimwood, Sarah

AU - Hutson, Peter H.

AU - Murray, Fraser

AU - Richards, Pawel

AU - Macaulay, Alison

AU - Wafford, Keith A.

PY - 2003/2

Y1 - 2003/2

N2 - Novel (E)-N1-(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 ∼1000-fold lower IC50 in NR2B than NR2A-containing cells. Replacement of the styryl unit by 2-naphthyl was well tolerated. © 2003 Elsevier Science Ltd. All rights reserved.

AB - Novel (E)-N1-(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 ∼1000-fold lower IC50 in NR2B than NR2A-containing cells. Replacement of the styryl unit by 2-naphthyl was well tolerated. © 2003 Elsevier Science Ltd. All rights reserved.

U2 - 10.1016/S0960-894X(02)01060-0

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

M3 - Article

C2 - 12639560

SN - 1464-3405

VL - 13

SP - 693

EP - 696

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 4

ER -

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

Abstract

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