Synthesis and SAR studies of 3-phenoxypropyl piperidine analogues as ORL1 (NOP) receptor agonists.

Palin, Ronald; Barn, David R; Clark, John K; Cottney, Jean E; Cowley, Phillip M; Crockatt, Marc; Evans, Louise; Feilden, Helen; Goodwin, Richard R; Griekspoor, Frank; Grove, Simon J A; Houghton, Andrea K; Jones, Philip S; Morphy, Richard J; Smith, Alasdair R C; Sundaram, Hardy; Vrolijk, David; Weston, Mark A; Wishart, Grant; Wren, Paul

Palin, Ronald; Barn, David R; Clark, John K; Cottney, Jean E; Cowley, Phillip M; Crockatt, Marc; Evans, Louise; Feilden, Helen; Goodwin, Richard R; Griekspoor, Frank; Grove, Simon J A; Houghton, Andrea K; Jones, Philip S; Morphy, Richard J; Smith, Alasdair R C; Sundaram, Hardy; Vrolijk, David; Weston, Mark A; Wishart, Grant; Wren, Paul.

Afiliação

Palin R; Department of Medicinal Chemistry, Organon Laboratories Ltd, Newhouse, Lanarkshire ML1 5SH, UK. r.palin@organon.co.uk

Bioorg Med Chem Lett ; 15(3): 589-93, 2005 Feb 01.

Article em En | MEDLINE | ID: mdl-15664818

RESUMO

A series of 3-phenoxypropyl piperidine analogues have been discovered as novel ORL1 receptor agonists. Structure-activity relationships have been explored around the 3-phenoxypropyl region with several potent and selective analogues identified.

Assuntos

Piperidinas/síntese química; Piperidinas/farmacologia; Receptores Opioides/agonistas; Animais; Células CHO; Cricetinae; AMP Cíclico/biossíntese; Desenho de Fármacos; Humanos; Interações Hidrofóbicas e Hidrofílicas; Concentração Inibidora 50; Masculino; Camundongos; Relação Estrutura-Atividade; Transfecção; Ducto Deferente; Receptor de Nociceptina

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Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piperidinas / Receptores Opioides Limite: Animals / Humans / Male Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2005 Tipo de documento: Article

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