title: SAR studies of 1,5-diarylpyrazole-based CCK1 receptor antagonists.
abstract: A high throughput screening campaign revealed compound 1 as a potent antagonist of the human CCK(1) receptor. Here, we report the syntheses and SAR studies of 1,5-diarylpyrazole analogs with various structural modifications of the alkane side chain of the molecule. The difference in affinity between the two enantiomers for the CCK(1) receptor and the flexible nature of the linker led to the design of constrained analogs with increased potency.
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA. lgomez4@prdus.jnj.com
authors.forename: Laurent
authors.initials: L
authors.lastname: Gomez
authors.forename: Michael D
authors.initials: MD
authors.lastname: Hack
authors.forename: Kelly
authors.initials: K
authors.lastname: McClure
authors.forename: Clark
authors.initials: C
authors.lastname: Sehon
authors.forename: Liming
authors.initials: L
authors.lastname: Huang
authors.forename: Magda
authors.initials: M
authors.lastname: Morton
authors.forename: Lina
authors.initials: L
authors.lastname: Li
authors.forename: Terrance D
authors.initials: TD
authors.lastname: Barrett
authors.forename: Nigel
authors.initials: N
authors.lastname: Shankley
authors.forename: J Guy
authors.initials: JG
authors.lastname: Breitenbucher
mesh_terms: D000818:Animals; D006801:Humans; D011720:Pyrazoles / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D043886:Receptor, Cholecystokinin A / Q000037:antagonists & inhibitors* / Q000502:physiology; D013329:Structure-Activity Relationship
chemical_list: D011720:Pyrazoles; D043886:Receptor, Cholecystokinin A