Pyridopyrimidine based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation.

Debenham, John S; Madsen-Duggan, Christina B; Wang, Junying; Tong, Xinchun; Lao, Julie; Fong, Tung M; Schaeffer, Marie-Therese; Xiao, Jing Chen; Huang, Cathy C R-R; Shen, Chun-Pyn; Sloan Stribling, D; Shearman, Lauren P; Strack, Alison M; Euan Macintyre, D; Hale, Jeffrey J; Walsh, Thomas F

Debenham, John S; Madsen-Duggan, Christina B; Wang, Junying; Tong, Xinchun; Lao, Julie; Fong, Tung M; Schaeffer, Marie-Therese; Xiao, Jing Chen; Huang, Cathy C R-R; Shen, Chun-Pyn; Sloan Stribling, D; Shearman, Lauren P; Strack, Alison M; Euan Macintyre, D; Hale, Jeffrey J; Walsh, Thomas F.

Afiliação

Debenham JS; Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA.

Bioorg Med Chem Lett ; 19(9): 2591-4, 2009 May 01.

Article em En | MEDLINE | ID: mdl-19328684

ABSTRACT

ABSTRACT

The synthesis, SAR and binding affinities are described for cannabinoid-1 receptor (CB1R) specific inverse agonists based on pyridopyrimidine and heterotricyclic scaffolds. Food intake and pharmacokinetic evaluation of several of these compounds indicate that they are effective orally active modulators of CB1R.

Assuntos

Agonistas de Receptores de Canabinoides; Obesidade/tratamento farmacológico; Pirimidinas/química; Administração Oral; Animais; Canabinoides/química; Química Farmacêutica/métodos; Desenho de Fármacos; Humanos; Concentração Inibidora 50; Estrutura Terciária de Proteína; Ratos; Receptor CB1 de Canabinoide/agonistas; Receptor CB2 de Canabinoide/agonistas; Relação Estrutura-Atividade

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirimidinas / Agonistas de Receptores de Canabinoides / Obesidade Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Ano de publicação: 2009 Tipo de documento: Article

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