title: Discovery of pyrimidine carboxamides as potent and selective CCK1 receptor agonists.
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.
authors.affiliation: Department of Medicinal Chemistry, Merck & Co. Inc., PO Box 2000, Rahway, NJ 07065, USA. liping_wang@merck.com
authors.forename: Liping
authors.initials: L
authors.lastname: Wang
authors.forename: James A
authors.initials: JA
authors.lastname: Hubert
authors.forename: Susan J
authors.initials: SJ
authors.lastname: Lee
authors.forename: Jie
authors.initials: J
authors.lastname: Pan
authors.forename: Su
authors.initials: S
authors.lastname: Qian
authors.forename: Marc L
authors.initials: ML
authors.lastname: Reitman
authors.forename: Alison M
authors.initials: AM
authors.lastname: Strack
authors.forename: Drew T
authors.initials: DT
authors.lastname: Weingarth
authors.forename: Douglas J
authors.initials: DJ
authors.lastname: MacNeil
authors.forename: Ann E
authors.initials: AE
authors.lastname: Weber
authors.forename: Scott D
authors.initials: SD
authors.lastname: Edmondson
mesh_terms: D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D002478:Cells, Cultured; D006571:Heterocyclic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D015394:Molecular Structure; D011485:Protein Binding / Q000187:drug effects; D011743:Pyrimidines / Q000737:chemistry; D043886:Receptor, Cholecystokinin A / Q000819:agonists*; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D006571:Heterocyclic Compounds; D011743:Pyrimidines; D043886:Receptor, Cholecystokinin A; C030986:pyrimidine