2. Academic Validation
  3. Synthesis and activity of 4,5-diarylimidazoles as human CB1 receptor inverse agonists

Synthesis and activity of 4,5-diarylimidazoles as human CB1 receptor inverse agonists

  • Bioorg Med Chem Lett. 2005 Mar 1;15(5):1441-6. doi: 10.1016/j.bmcl.2004.12.078.
Christopher W Plummer 1,  Paul E Finke,  Sander G Mills,  Junying Wang,  Xinchun Tong,  George A Doss,  Tung M Fong,  Julie Z Lao,  Marie-Therese Schaeffer,  Jing Chen,  Chun-Pyn Shen,  D Sloan Stribling,  Lauren P Shearman,  Alison M Strack,  Lex H T Van der Ploeg
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. christopher_plummer@merck.com
PMID: 15713403 DOI: 10.1016/j.bmcl.2004.12.078
Abstract

Structure-activity relationship studies directed toward the optimization of 4,5-diarylimidazole-2-carboxamide analogs as human CB1 receptor inverse agonists resulted in the discovery of the two amide derivatives 24a and b (hCB1 IC50 = 6.1 and 4.0 nM) which also demonstrated efficacy in overnight feeding studies in the rat for reduction in both food intake and overall body weight.

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