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Bioorg Med Chem Lett. 2008 Sep 1;18(17):4833-7. doi: 10.1016/j.bmcl.2008.07.083. Epub 2008 Jul 24.

2-Substituted piperazine-derived imidazole carboxamides as potent and selective CCK1R agonists for the treatment of obesity.

Author information

1
Department of Medicinal Chemistry, Merck & Co., Inc., 126 East Lincoln Ave., PO Box 2000, Rahway, NJ 07065-0900, USA.

Abstract

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.

PMID:
18684621
DOI:
10.1016/j.bmcl.2008.07.083
[Indexed for MEDLINE]

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