[Studies on the synthesis of cholecystokinin A receptor antagonists. I. synthesis and cholecystokinin A receptor inhibitory activities of malonamide derivatives].
2-Substituted malonamide derivatives were synthesized and tested for cholecystokinin A (CCK-A) receptor inhibitory activity. Significant CCK-A receptor inhibitory activities were found in only three compounds (4g-i) which have carboxyl group. In order to study structure-activity relationships, carboxyethyl group was selected for 2-substituent and a number of N-substituted malonamides were prepared. After these compounds were tested for CCK-A receptor inhibitory activity, 4-(3,4-dichlorophenylcarbamoyl)-N,N-dipentylglutaramic acid (4h) was selected as the most preferred compound.
Ajisawa
Y
Y
Central Research Laboratories, Kissei Pharmaceutical Co. Ltd., Kashiwabara, Nagano, Japan.
Kitazawa
M
M
Uchida
M
M
Kobayashi
M
M
D008314:Malonates / Q000138:chemical synthesis* / Q000494:pharmacology; D011949:Receptors, Cholecystokinin / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D008314:Malonates; D011949:Receptors, Cholecystokinin; C008314:malonamide