Dihydro-pyrano[2,3-b]pyridines and tetrahydro-1,8-naphthyridines as CB1 receptor inverse agonists: Synthesis,SAR and biological evaluation |
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| Authors: | Christina B. Madsen-Duggan John S. Debenham Thomas F. Walsh Lin Yan Pei Huo Junying Wang Xinchun Tong Julie Lao Tung M. Fong Jing Chen Xiao Cathy R.-R.C. Huang Chun-Pyn Shen D.Sloan Stribling Lauren P. Shearman Alison M. Strack Mark T. Goulet Jeffrey J. Hale |
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| Affiliation: | 1. Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA;2. Department of Metabolic Disorders, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA;3. Department of Pharmacology, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA |
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| Abstract: | Synthesis and structure–activity relationships of cannabinoid-1 receptor (CB1R) inverse agonists based on dihydro-pyrano[2,3-b] pyridine and tetrahydro-1,8-naphtyridine scaffolds are presented. Rat food intake and pharmacokinetic evaluation of 13g, 13i, 13k and 17a revealed these compounds to be highly efficacious orally active modulators of CB1R. |
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