Title of article
Synthesis and activity of 4,5-diarylimidazoles as human CB1 receptor inverse agonists
Author/Authors
Christopher W. Plummer، نويسنده , , Paul E. Finke، نويسنده , , Sander G. Mills، نويسنده , , Junying Wang، نويسنده , , Xinchun Tong، نويسنده , , George A. Doss، نويسنده , , Tung M. Fong، نويسنده , , Julie Z. Lao، نويسنده , , Marie-Therese Schaeffer، نويسنده , , Jing Chen، نويسنده , , Chun-Pyn Shen، نويسنده , , D. Sloan Stribling، نويسنده , , Lauren P. Shearman، نويسنده , , Alison M. Strack، نويسنده , , Lex H.T. Van der Ploeg، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
6
From page
1441
To page
1446
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.
Keywords
obesity , CB1 inverse agonist , cannabinoid , Imidazole
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795412
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