Potent and subtype-selective CCK-B/gastrin receptor antagonists: 2, 4-dioxo-1, 5-benzodiazepines with a plane of symmetry

…, N Haga, Y Ishihara, M Ishikawa, M Shimamura

Index: Hagishita, Sanji; Seno, Kaoru; Kamata, Susumu; Haga, Nobuhiro; Ishihara, Yasunobu; Ishikawa, Michio; Shimamura, Mayumi Bioorganic and Medicinal Chemistry, 1997 , vol. 5, # 7 p. 1433 - 1446

Full Text: HTML

Citation Number: 18

Abstract

A series of CCK-B/gastrin receptor antagonists, 2, 4-dioxo-1, 5-benzodiazepine derivatives with a plane of symmetry, were designed, synthesized, and evaluated for antagonistic activity. Structure-activity relationship studies revealed that carbonylmethyl groups at both N- 1 and N-5 positions and hydrophilic groups, such as the carboxyl group on the benzene ring attached to the ureido group at the C-3 position, brought about potent affinity and subtype ...