Synthesis and SAR of New 5-Phenyl-3-ureido-1,5-benzodiazepines as Cholecystokinin-B Receptor Antagonists
2000
A series of 5-phenyl-3-ureidobenzodiazepine-2,4-diones was synthesized and evaluated as cholecystokinin-B (CCK-B) receptor antagonists. Structure-activity relationship (SAR) studies revealed the importance of the N-1 substituent for potent and selective CCK-B affinity. Addition of substituents at the urea side chain provided in some cases more potent compounds. Moreover the introduction of bulky substituents such as adamantylmethyl at N-1 and resolution of the racemic ureas resulted in our lead compound GV150013.
Keywords:
- Correction
- Source
- Cite
- Save
- Machine Reading By IdeaReader
37
References
47
Citations
NaN
KQI