Discovery of pyrimidine carboxamides as potent and selective CCK1 receptor agonists

Liping Wang; James A Hubert; Susan J Lee; Jie Pan; Su Qian; Marc L Reitman; Alison M Strack; Drew T Weingarth; Douglas J MacNeil; Ann E Weber; Scott D Edmondson

doi:10.1016/j.bmcl.2011.03.069

Discovery of pyrimidine carboxamides as potent and selective CCK1 receptor agonists

Bioorg Med Chem Lett. 2011 May 15;21(10):2911-5. doi: 10.1016/j.bmcl.2011.03.069. Epub 2011 Mar 31.

Authors

Liping Wang¹, James A Hubert, Susan J Lee, Jie Pan, Su Qian, Marc L Reitman, Alison M Strack, Drew T Weingarth, Douglas J MacNeil, Ann E Weber, Scott D Edmondson

Affiliation

¹ Department of Medicinal Chemistry, Merck & Co. Inc., PO Box 2000, Rahway, NJ 07065, USA. liping_wang@merck.com

PMID: 21493064
DOI: 10.1016/j.bmcl.2011.03.069

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.

MeSH terms

Amides / chemical synthesis*
Amides / chemistry
Amides / pharmacology*
Animals
Cells, Cultured
Heterocyclic Compounds / chemical synthesis
Heterocyclic Compounds / chemistry
Heterocyclic Compounds / pharmacology
Humans
Inhibitory Concentration 50
Mice
Molecular Structure
Protein Binding / drug effects
Pyrimidines / chemistry
Receptor, Cholecystokinin A / agonists*
Structure-Activity Relationship

Substances

Amides
Heterocyclic Compounds
Pyrimidines
Receptor, Cholecystokinin A
pyrimidine