Potent achiral agonists of the ghrelin (growth hormone secretagogue) receptor. Part I: Lead identification.

Heightman, Tom D; Scott, Jackie S; Longley, Mark; Bordas, Vincent; Dean, David K; Elliott, Richard; Hutley, Gail; Witherington, Jason; Abberley, Lee; Passingham, Barry; Berlanga, Manuela; de Los Frailes, Maite; Wise, Alan; Powney, Ben; Muir, Alison; McKay, Fiona; Butler, Sharon; Winborn, Kim; Gardner, Christopher; Darton, Jill; Campbell, Colin; Sanger, Gareth

Heightman, Tom D; Scott, Jackie S; Longley, Mark; Bordas, Vincent; Dean, David K; Elliott, Richard; Hutley, Gail; Witherington, Jason; Abberley, Lee; Passingham, Barry; Berlanga, Manuela; de Los Frailes, Maite; Wise, Alan; Powney, Ben; Muir, Alison; McKay, Fiona; Butler, Sharon; Winborn, Kim; Gardner, Christopher; Darton, Jill; Campbell, Colin; Sanger, Gareth.

Afiliação

Heightman TD; Department of Medicinal Chemistry & DMPK, Neurology & GI Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. Tom.D.Heightman@gsk.com

Bioorg Med Chem Lett ; 17(23): 6584-7, 2007 Dec 01.

Article em En | MEDLINE | ID: mdl-17942309

ABSTRACT

ABSTRACT

High throughput screening combined with efficient datamining and parallel synthesis led to the discovery of a novel series of indolines showing potent in vitro ghrelin receptor agonist activity and acceleration of gastric emptying in rats.

Assuntos

Indóis/química; Receptores de Grelina/agonistas; Animais; Esvaziamento Gástrico/efeitos dos fármacos; Esvaziamento Gástrico/fisiologia; Hormônio do Crescimento Humano/agonistas; Humanos; Indóis/farmacologia; Ratos; Receptores de Grelina/fisiologia; Estereoisomerismo

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Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Receptores de Grelina / Indóis Tipo de estudo: Diagnostic_studies Limite: Animals / Humans Idioma: En Ano de publicação: 2007 Tipo de documento: Article

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