Synthesis and activity of 4,5-diarylimidazoles as human CB1 receptor inverse agonists.
作者信息
Plummer Christopher W, Finke Paul E, Mills Sander G, Wang Junying, Tong Xinchun, Doss George A, Fong Tung M, Lao Julie Z, Schaeffer Marie-Therese, Chen Jing, Shen Chun-Pyn, Stribling D Sloan, Shearman Lauren P, Strack Alison M, Van der Ploeg Lex H T
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 2005 Mar 1;15(5):1441-6. doi: 10.1016/j.bmcl.2004.12.078.
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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