Literature DB >> 15713403

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

Christopher W Plummer1, 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.   

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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Year:  2005        PMID: 15713403     DOI: 10.1016/j.bmcl.2004.12.078

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

Review 1.  Pharmacotherapeutic targeting of the endocannabinoid signaling system: drugs for obesity and the metabolic syndrome.

Authors:  V Kiran Vemuri; David R Janero; Alexandros Makriyannis
Journal:  Physiol Behav       Date:  2007-11-21
  1 in total

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