title: Discovery of imidazole carboxamides as potent and selective CCK1R agonists.
abstract: High-throughput screening revealed diaryl pyrazole 3 as a selective albeit modest cholecystokinin 1 receptor (CCK1R) agonist. SAR studies led to the discovery and optimization of a novel class of 1,2-diaryl imidazole carboxamides. Compound 44, which was profiled extensively, showed good in vivo mouse gallbladder emptying (mGBE) and lean mouse overnight food intake (ONFI) reduction activities.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co. Inc., PO Box 2000, Rahway, NJ 07065, USA. cheng_zhu@merck.com
authors.forename: Cheng
authors.initials: C
authors.lastname: Zhu
authors.forename: Alexa R
authors.initials: AR
authors.lastname: Hansen
authors.forename: Thomas
authors.initials: T
authors.lastname: Bateman
authors.forename: Zhesheng
authors.initials: Z
authors.lastname: Chen
authors.forename: Tom G
authors.initials: TG
authors.lastname: Holt
authors.forename: James A
authors.initials: JA
authors.lastname: Hubert
authors.forename: Bindhu V
authors.initials: BV
authors.lastname: Karanam
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: Vijay B G
authors.initials: VB
authors.lastname: Reddy
authors.forename: Marc L
authors.initials: ML
authors.lastname: Reitman
authors.forename: Alison M
authors.initials: AM
authors.lastname: Strack
authors.forename: Vincent
authors.initials: V
authors.lastname: Tong
authors.forename: Drew T
authors.initials: DT
authors.lastname: Weingarth
authors.forename: Michael S
authors.initials: MS
authors.lastname: Wolff
authors.forename: Doug J
authors.initials: DJ
authors.lastname: MacNeil
authors.forename: Ann E
authors.initials: AE
authors.lastname: Weber
authors.forename: Joseph L
authors.initials: JL
authors.lastname: Duffy
authors.forename: Scott D
authors.initials: SD
authors.lastname: Edmondson
mesh_terms: D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D019440:Anti-Obesity Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D019742:Chemokines, CC; D020650:Combinatorial Chemistry Techniques; D004435:Eating / Q000187:drug effects; D016473:Gallbladder Emptying / Q000187:drug effects; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D051379:Mice; D015394:Molecular Structure; D011949:Receptors, Cholecystokinin / Q000819:agonists*; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D019440:Anti-Obesity Agents; C511142:Ccl28 protein, mouse; D019742:Chemokines, CC; D007093:Imidazoles; D011949:Receptors, Cholecystokinin