[Studies on the synthesis of cholecystokinin A receptor antagonists. IV. Synthesis and cholecystokinin A receptor inhibitory activities of benzimidazole derivatives].
A number of benzimidazole 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 the compounds having carboxyl or tetrazolyl group. As the most preferred compound, 4-(5,6-dichlorobenzimidazol-2-yl)-N-(3-methoxypropyl)-N-pentylg lutaramic acid (4g) was selected.
Ajisawa
Y
Y
Central Research Laboratories, Kissei Pharmaceutical Co. Ltd., Nagano, Japan.
Akahane
K
K
Akahane
M
M
Sato
K
K
Tamai
T
T
Saito
M
M
Tanaka
N
N
Kamata
K
K
Kobayashi
M
M
D000478:Alkylation; D000818:Animals; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D006868:Hydrolysis; 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
D001562:Benzimidazoles; D043886:Receptor, Cholecystokinin A; D011949:Receptors, Cholecystokinin; C031000:benzimidazole