| 18684621 |
Berger R, Zhu C, Hansen AR, Harper B, Chen Z, Holt TG, Hubert J, Lee SJ, Pan J, Qian S, Reitman ML, Strack AM, Weingarth DT, Wolff M, Macneil DJ, Weber AE, Edmondson SD: 2-Substituted piperazine-derived imidazole carboxamides as potent and selective CCK1R agonists for the treatment of obesity. Bioorg Med Chem Lett. 2008 Sep 1;18(17):4833-7. Epub 2008 Jul 24.
The discovery and structure-activity relationship of 1,2-diarylimidazole piperazine carboxamides bearing polar side chains as potent and selective cholecystokinin 1 receptor (CCK1R) agonists are described. Optimization of this series resulted in the discovery of isopropyl carboxamide 40, a CCK1R agonist with sub-nanomolar functional and binding activity as well as excellent potency in a mouse overnight food intake reduction assay. |
31(0,1,1,1) |