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. 2000 Oct 5;43(20):3596-613.
doi: 10.1021/jm990967h.

Synthesis and SAR of new 5-phenyl-3-ureido-1,5-benzodiazepines as cholecystokinin-B receptor antagonists

A Ursini  1 , A M Capelli, R A Carr, P Cassarà, M Corsi, O Curcuruto, G Curotto, M Dal Cin, S Davalli, D Donati, A Feriani, H Finch, G Finizia, G Gaviraghi, M Marien, G Pentassuglia, S Polinelli, E Ratti, A M Reggiani, G Tarzia, G Tedesco, M E Tranquillini, D G Trist, F T Van Amsterdam
Affiliations

Synthesis and SAR of new 5-phenyl-3-ureido-1,5-benzodiazepines as cholecystokinin-B receptor antagonists

A Ursini et al. J Med Chem. .

Erratum in

  • J Med Chem 2000 Dec 28;43(26):5057. Reggiani A [corrected to Reggiani AM]

Abstract

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.

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