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Synthesis and SAR of New 5-Phenyl-3-ureido-1,5-benzodiazepines as Cholecystokinin-B Receptor Antagonists

2000; American Chemical Society; Volume: 43; Issue: 20 Linguagem: Inglês

10.1021/jm990967h

1520-4804

Antonella Ursini, Anna Maria Capelli, Robin A. E. Carr, Paolo G. Cassarà, Mauro Corsi, Ornella Curcuruto, Giovanni Curotto, Michele Dal Cin, Silvia Davalli, Daniele Donati, Aldo Feriani, Harry Finch, Gabriella Finizia, G. Gaviraghi, Marc Marien, Giorgio Pentassuglia, Stefano Polinelli, Emiliangelo Ratti, Aldo Reggiani, Giorgio Tarzia, Giovanna Tedesco, Maria Elvira Tranquillini, David G. Trist, F. Th. M. van Amsterdam,

Pharmacological Effects of Natural Compounds

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.