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Furo[2,3-b]pyridine-based cannabinoid-1 receptor inverse agonists: synthesis and biological evaluation. Part 1.
Debenham, John S; Madsen-Duggan, Christina B; Toupence, Richard B; Walsh, Thomas F; Wang, Junying; Tong, Xinchun; Kumar, Sanjeev; Lao, Julie; Fong, Tung M; Xiao, Jing Chen; Huang, Cathy R-R C; Shen, Chun-Pyn; Feng, Yue; Marsh, Donald J; Stribling, D Sloan; Shearman, Lauren P; Strack, Alison M; Goulet, Mark T.
Afiliação
  • Debenham JS; Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. john_debenham@merck.com
Bioorg Med Chem Lett ; 20(4): 1448-52, 2010 Feb 15.
Article em En | MEDLINE | ID: mdl-20096577
ABSTRACT
The synthesis, SAR and binding affinities of cannabinoid-1 receptor (CB1R) inverse agonists based on furo[2,3-b]pyridine scaffolds are described. Food intake, mechanism specific efficacy, pharmacokinetic, and metabolic evaluation of several of these compounds indicate that they are effective orally active modulators of CB1R.
Assuntos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piridinas / Desenho de Fármacos / Receptor CB1 de Canabinoide / Furanos Limite: Animals / Humans Idioma: En Ano de publicação: 2010 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piridinas / Desenho de Fármacos / Receptor CB1 de Canabinoide / Furanos Limite: Animals / Humans Idioma: En Ano de publicação: 2010 Tipo de documento: Article