STUDIES ON THE SYNTHESIS OF CHOLECYSTOKIN IN-A RECEPTOR ANTAGONISTS .1. SYNTHESIS AND CHOLECYSTOKININ-A RECEPTOR INHIBITORY ACTIVITIES OF MALONAMIDE DERIVATIVES

2-Substituted malonamide derivatives were synthesized and tested for c holecystokinin A (CCK-A) receptor inhibitory activity. Significant CCK -B 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 compou nds were tested for CCK-A receptor inhibitory activity, ,4-dichlorophe nylcarbamoyl)-N,N-dipentylglutaramic acid (4h) was selected as the mos t preferred compound.