[Studies on the synthesis of cholecystokinin A receptor antagonists. III. Synthesis and cholecystokinin A receptor inhibitory activities of naphthyl sulfone derivatives].
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.
Ajisawa
Y
Y
Central Research Laboratories, Kissei Pharmaceutical Co., Ltd., Nagano, Japan.
Kitazawa
M
M
Nakano
Y
Y
Tsubaki
A
A
Ban
M
M
Sato
K
K
Okazaki
K
K
Uchida
M
M
Kobayashi
M
M
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
D009281:Naphthalenes; D043886:Receptor, Cholecystokinin A; D011949:Receptors, Cholecystokinin; D013450:Sulfones