170855-49-9

Upstream product

• 95-54-5 1,2-diamino-benzene 
• 621-29-4 3-tolyl isocyanate 
• 170856-14-1 1,5-dihydrobenzo[b][1,4]diazepine-2,3,4-trione 3-(O-methyloxime) 
• 170856-32-3 3-amino-1H-1,5-benzodiazepine-2,4-(3H,5H)-dione 
• 170856-15-2 3-[N'-(m-tolyl)ureido]-1H-1,5-benzodiazepine-2,4-(3H,5H)-dione 

Relevant academic research and scientific papers

Benzodiazepine derivative

A benzodiazepine derivative of the formula (I): STR1 wherein R 1 is a bond, --CH 2 --, --CH 2 O--, --SCH 2 -- or a group of the formula: STR2 R 2 is a lower alkyl, --COOR 5, --CONH(CH 2) n COOR 5, --CONHSO 2 R 5, --SO 2 NHCOR 5, or an optionally substituted heterocyclic group (R 5 is a hydrogen atom, lower alkyl or benzyl and n is an integer of 1 to 5); R 3 is a bond, --CO-- or --CONH--; and R 4 is an optionally substituted heterocyclic group, optionally substituted lower alkyl, optionally substituted lower cycloalkyl, optionally substituted aryl, or lower alkoxycarbonyl group, or a pharmaceutically acceptable salt thereof, which has a high affinity for gastrin receptors and/or CCK-B receptors but not for CCK-A receptors, and is useful for treating diseases associated with gastrin receptors and/or CCK-B receptors without inducing the side effects associated with CCK-A receptors.

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

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 selectivity for CCK-B/gastrin receptors. Several compounds showed excellent in vivo inhibition of gastric acid secretion induced by pentagastrin in anesthetized rats.