Rapid access towards follow-up NOP receptor agonists using a knowledge based approach.

Palin, Ronald; Clark, John K; Evans, Louise; Feilden, Helen; Fletcher, Dan; Hamilton, Niall M; Houghton, Andrea K; Jones, Philip S; McArthur, Duncan; Montgomery, Brian; Ratcliffe, Paul D; Smith, Alasdair R C; Sutherland, Aaron; Weston, Mark A; Wishart, Grant

Palin, Ronald; Clark, John K; Evans, Louise; Feilden, Helen; Fletcher, Dan; Hamilton, Niall M; Houghton, Andrea K; Jones, Philip S; McArthur, Duncan; Montgomery, Brian; Ratcliffe, Paul D; Smith, Alasdair R C; Sutherland, Aaron; Weston, Mark A; Wishart, Grant.

Afiliação

Palin R; Department of Chemistry, Schering-Plough Research Institute, Newhouse, Lanarkshire ML15SH, UK. ronald.palin@spcorp.com

Bioorg Med Chem Lett ; 19(22): 6441-6, 2009 Nov 15.

Article em En | MEDLINE | ID: mdl-19818611

ABSTRACT

ABSTRACT

A knowledge based approach has been adopted to identify novel NOP receptor agonists with simplified hydrophobes. Substitution of the benzimidazol-2-one piperidine motif with a range of hydrophobic groups and pharmacophore guided bio-isosteric replacement of the benzimidazol-2-one moiety was explored. Compound 51 was found to be a high affinity, potent NOP receptor agonist with reduced affinity for the hERG channel.

Assuntos

Benzimidazóis/química; Antagonistas de Entorpecentes/química; Piperidinas/química; Animais; Cricetinae; Receptores Opioides/metabolismo; Relação Estrutura-Atividade; Receptor de Nociceptina

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piperidinas / Benzimidazóis / Antagonistas de Entorpecentes Limite: Animals Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2009 Tipo de documento: Article País de afiliação: Reino Unido

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