title: Synthesis of phenoxyacetic acid derivatives as highly potent antagonists of gastrin/cholecystokinin-B receptors.
abstract: A novel series of phenoxyacetic acid derivatives was synthesized based on considerations of the three-dimensional structural similarity of YM022 and RP72540. The gastrin/cholecystokinin (CCK)-B and CCK-A receptor antagonist activities of these compounds were evaluated by investigation of their affinities for human gastrin/CCK-B receptors and human CCK-A receptors, respectively. It was found that N-methyl-N-phenyl-2-[2-[N-(N-methyl-N-phenyl-carbamoylmethyl)-N-[2 -[3-(3- methylphenyl)ureido]acetyl]amino]phenoxy]acetamide (20k, DZ-3514) exhibited high affinity for gastrin/CCK-B receptors and high selectivity over CCK-A receptors.
authors.affiliation: New Product Research Laboratories III, Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan.
authors.forename: Y
authors.initials: Y
authors.lastname: Takeda
authors.forename: K
authors.initials: K
authors.lastname: Kawagoe
authors.forename: A
authors.initials: A
authors.lastname: Yokomizo
authors.forename: Y
authors.initials: Y
authors.lastname: Yokomizo
authors.forename: T
authors.initials: T
authors.lastname: Hosokami
authors.forename: Y
authors.initials: Y
authors.lastname: Ogihara
authors.forename: Y
authors.initials: Y
authors.lastname: Honda
authors.forename: S
authors.initials: S
authors.lastname: Yokohama
mesh_terms: D000081:Acetamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D016466:CHO Cells / Q000187:drug effects; D002766:Cholecystokinin / Q000037:antagonists & inhibitors* / Q000187:drug effects; D006224:Cricetinae; D005755:Gastrins / Q000037:antagonists & inhibitors* / Q000187:drug effects; D018014:Gene Transfer Techniques; D006801:Humans; D010671:Phenylurea Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000081:Acetamides; C111699:DZ 3514; D005755:Gastrins; D010671:Phenylurea Compounds; D002766:Cholecystokinin