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Lead optimization of 5,6-diarylpyridines as CB1 receptor inverse agonists.
Madsen-Duggan, Christina B; Debenham, John S; Walsh, Thomas F; Toupence, Richard B; Huang, Song X; Wang, Junying; Tong, Xinchun; Lao, Julie; Fong, Tung M; Schaeffer, Marie-Therese; Xiao, Jing Chen; Huang, Cathy R-R C; Shen, Chun-Pyn; Stribling, D Sloan; Shearman, Lauren P; Strack, Alison M; MacIntyre, D Euan; Van der Ploeg, Lex H T; Goulet, Mark T.
Afiliação
  • Madsen-Duggan CB; Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. christina_madsen_duggan@merck.com
Bioorg Med Chem Lett ; 17(7): 2031-5, 2007 Apr 01.
Article em En | MEDLINE | ID: mdl-17270441
ABSTRACT
Optimization of the biological activity for 5,6-diarylpyridines as CB1 receptor inverse agonists is described. Food intake and pharmacokinetic evaluation of 3f and 15c indicate that these compounds are effective orally active modulators of CB1.
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Base de dados: MEDLINE Assunto principal: Piridinas / Química Farmacêutica / Receptor CB1 de Canabinoide Idioma: En Ano de publicação: 2007 Tipo de documento: Article
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Base de dados: MEDLINE Assunto principal: Piridinas / Química Farmacêutica / Receptor CB1 de Canabinoide Idioma: En Ano de publicação: 2007 Tipo de documento: Article