Article

Discovery of pyrimidine carboxamides as potent and selective CCK1 receptor agonists.

Department of Medicinal Chemistry, Merck & Co. Inc., PO Box 2000, Rahway, NJ 07065, USA.
Bioorganic & medicinal chemistry letters (impact factor: 2.65). 05/2011; 21(10):2911-5. DOI:10.1016/j.bmcl.2011.03.069
Source: PubMed

ABSTRACT A series of six-membered heterocycle carboxamides were synthesized and evaluated as cholecystokinin 1 receptor (CCK1R) agonists. A pyrimidine core proved to be the best heterocycle, and SAR studies resulted in the discovery of analog 5, a potent and structurally diverse CCK1R agonist.

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Keywords

analog 5
 
CCK1R
 
cholecystokinin 1 receptor
 
pyrimidine core
 
six-membered heterocycle carboxamides
 
structurally diverse CCK1R agonist