title: [Studies on the synthesis of cholecystokinin A receptor antagonists. III. Synthesis and cholecystokinin A receptor inhibitory activities of naphthyl sulfone derivatives].
abstract: A number of naphthyl sulfone derivatives were synthesized and tested for cholecystokinin A (CCK-A) receptor inhibitory activity in order to study structure-activity relationships. Significant CCK-A receptor inhibitory activities were found in sulfone-carboxylic acid derivatives (7) having very hydrophobic sidechains. As the most preferred compound, (R)-4-[N-(3-methoxypropyl)-N-pentylcarbamoyl]-5-(2-naphthylsulf onyl) pentanoic acid ((R)-7c) was selected.
authors.affiliation: Central Research Laboratories, Kissei Pharmaceutical Co., Ltd., Nagano, Japan.
authors.forename: Y
authors.initials: Y
authors.lastname: Ajisawa
authors.forename: M
authors.initials: M
authors.lastname: Kitazawa
authors.forename: Y
authors.initials: Y
authors.lastname: Nakano
authors.forename: A
authors.initials: A
authors.lastname: Tsubaki
authors.forename: M
authors.initials: M
authors.lastname: Ban
authors.forename: K
authors.initials: K
authors.lastname: Sato
authors.forename: K
authors.initials: K
authors.lastname: Okazaki
authors.forename: M
authors.initials: M
authors.lastname: Uchida
authors.forename: M
authors.initials: M
authors.lastname: Kobayashi
mesh_terms: D000818:Animals; D066298:In Vitro Techniques; D008297:Male; D009281:Naphthalenes / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D043886:Receptor, Cholecystokinin A; D011949:Receptors, Cholecystokinin / Q000037:antagonists & inhibitors* / Q000737:chemistry; D013329:Structure-Activity Relationship; D013450:Sulfones / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D009281:Naphthalenes; D043886:Receptor, Cholecystokinin A; D011949:Receptors, Cholecystokinin; D013450:Sulfones