2. Academic Validation
  3. Synthesis of functionalized 1,8-naphthyridinones and their evaluation as novel, orally active CB1 receptor inverse agonists

Synthesis of functionalized 1,8-naphthyridinones and their evaluation as novel, orally active CB1 receptor inverse agonists

  • Bioorg Med Chem Lett. 2006 Feb;16(3):681-5. doi: 10.1016/j.bmcl.2005.10.028.
John S Debenham 1,  Christina B Madsen-Duggan,  Thomas F Walsh,  Junying Wang,  Xinchun Tong,  George A Doss,  Julie Lao,  Tung M Fong,  Marie-Therese Schaeffer,  Jing Chen Xiao,  Cathy R-R C Huang,  Chun-Pyn Shen,  Yue Feng,  Donald J Marsh,  D Sloan Stribling,  Lauren P Shearman,  Alison M Strack,  D Euan MacIntyre,  Lex H T Van der Ploeg,  Mark T Goulet
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. [email protected]
PMID: 16263284 DOI: 10.1016/j.bmcl.2005.10.028
Abstract

Synthesis, SAR, and binding affinities are described for a new class of 1,8-naphthyridinone CB1 receptor specific inverse agonists. Food intake, knockout mouse, and pharmacokinetic evaluation of 14 indicate that this compound is an effective orally active modulator of CB1.

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