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Lead optimization of 5,6-diarylpyridines as CB1 receptor inverse agonists |
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| Authors: | 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 |
| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. christina_madsen_duggan@merck.com |
| 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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