title: Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists I: discovery of CCKR1 selectivity in a previously CCKR2-selective lead series.
abstract: A series of CCK2R-selective anthranilic amides is shown to derive CCK1R affinity via selective substitution of the amide side chain. Thus, extending the length of the original benzamide side chain by a single methylene unit imparts CCK1R affinity to the series, and further fine tuning of the affinity results in CCK1R selectivity of greater than 100-fold.
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
authors.forename: Marna
authors.initials: M
authors.lastname: Pippel
authors.forename: Brett D
authors.initials: BD
authors.lastname: Allison
authors.forename: Victor K
authors.initials: VK
authors.lastname: Phuong
authors.forename: Lina
authors.initials: L
authors.lastname: Li
authors.forename: Magda F
authors.initials: MF
authors.lastname: Morton
authors.forename: Clodagh
authors.initials: C
authors.lastname: Prendergast
authors.forename: Xiaodong
authors.initials: X
authors.lastname: Wu
authors.forename: Nigel P
authors.initials: NP
authors.lastname: Shankley
authors.forename: Michael H
authors.initials: MH
authors.lastname: Rabinowitz
mesh_terms: D000818:Animals; D001549:Benzamides / Q000494:pharmacology; D003001:Cloning, Molecular; D004353:Drug Evaluation, Preclinical; D005838:Genotype; D007555:Isoxazoles / Q000737:chemistry*; D018782:Maze Learning; D008958:Models, Molecular; D051381:Rats; D017207:Rats, Sprague-Dawley; D043886:Receptor, Cholecystokinin A / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism; D043887:Receptor, Cholecystokinin B / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000494:pharmacology*
chemical_list: D001549:Benzamides; D007555:Isoxazoles; D043886:Receptor, Cholecystokinin A; D043887:Receptor, Cholecystokinin B; D013449:Sulfonamides; C033962:anthranil; C037689:benzamide