The discovery of GSK221149A: a potent and selective oxytocin antagonist.

Liddle, John; Allen, Michael J; Borthwick, Alan D; Brooks, David P; Davies, David E; Edwards, Richard M; Exall, Anne M; Hamlett, Chris; Irving, Wendy R; Mason, Andrew M; McCafferty, Gerald P; Nerozzi, Fabrizio; Peace, Simon; Philp, Joanne; Pollard, Derek; Pullen, Mark A; Shabbir, Shaila S; Sollis, Steve L; Westfall, Timothy D; Woollard, Pat M; Wu, Charlene; Hickey, Deirdre M B

Liddle, John; Allen, Michael J; Borthwick, Alan D; Brooks, David P; Davies, David E; Edwards, Richard M; Exall, Anne M; Hamlett, Chris; Irving, Wendy R; Mason, Andrew M; McCafferty, Gerald P; Nerozzi, Fabrizio; Peace, Simon; Philp, Joanne; Pollard, Derek; Pullen, Mark A; Shabbir, Shaila S; Sollis, Steve L; Westfall, Timothy D; Woollard, Pat M; Wu, Charlene; Hickey, Deirdre M B.

Afiliação

Liddle J; Department of Medicinal Chemistry, GlaxoSmithKline Research and Development, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, UK. john.2.liddle@gsk.com

Bioorg Med Chem Lett ; 18(1): 90-4, 2008 Jan 01.

Article em En | MEDLINE | ID: mdl-18032036

ABSTRACT

ABSTRACT

Optimisation of a series of oxazole diketopiperazines has led to the discovery of a very potent and selective oxytocin antagonist GSK221149A. GSK221149A has been shown to inhibit oxytocin-induced uterine contractions in the anaesthetised rat.

Assuntos

Ocitocina/antagonistas & inibidores; Piperazinas/química; Piperazinas/farmacologia; Animais; Feminino; Humanos; Cinética; Ocitocina/metabolismo; Piperazinas/farmacocinética; Ratos; Ratos Sprague-Dawley; Receptores de Ocitocina/metabolismo; Relação Estrutura-Atividade; Contração Uterina/efeitos dos fármacos

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Base de dados: MEDLINE Assunto principal: Piperazinas / Ocitocina Limite: Animals / Female / Humans Idioma: En Ano de publicação: 2008 Tipo de documento: Article

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Imprimir

XML

PubMed Links

Base de dados: MEDLINE Assunto principal: Piperazinas / Ocitocina Limite: Animals / Female / Humans Idioma: En Ano de publicação: 2008 Tipo de documento: Article