[Studies on the synthesis of cholecystokinin A receptor antagonists. II. Synthesis and cholecystokinin A receptor inhibitory activities of sulfur-containing amide-carboxylic acid derivatives].
A number of sulfur-containing amide-carboxylic acid 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 only two series, that is, sulfoxide-carboxylic acid derivatives (9) and sulfone-carboxylic acid derivatives (10). As the most preferred compound, 5-(3,4-dichlorophenylsulfonyl)-4-(N,N-dipentylcarbamoyl)pent anoic acid (10n) 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
Kobayashi
M
M
D000818:Animals; D066298:In Vitro Techniques; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D043886:Receptor, Cholecystokinin A; D011949:Receptors, Cholecystokinin / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013440:Sulfides / Q000494:pharmacology*; D013450:Sulfones / Q000494:pharmacology*; D013454:Sulfoxides / Q000494:pharmacology*
D043886:Receptor, Cholecystokinin A; D011949:Receptors, Cholecystokinin; D013440:Sulfides; D013450:Sulfones; D013454:Sulfoxides