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
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA.
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.
