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Bioorg Med Chem ; 19(14): 4257-73, 2011 Jul 15.
Article in English | MEDLINE | ID: mdl-21689940

ABSTRACT

This article deals with the synthesis and the activities of some 1,5-dialkyl-3-arylureido-1,5-benzodiazepin-2,4-diones which were prepared as potential CCK2 antagonists, with the intention to find a possible follow up of our lead compound GV150013, showing an improved pharmacokinetic profile. The phenyl ring at N-5 was replaced with more hydrophilic substituents, like alkyl groups bearing basic functions. In some cases, the resolution of the racemic key intermediates 3-amino-benzodiazepines was also accomplished. Among the compounds synthesized and characterised so far in this class, the 5-morpholinoethyl derivative 54, was selected as potential follow up of GV150013 and submitted for further evaluation.


Subject(s)
Benzodiazepinones/pharmacology , Receptor, Cholecystokinin B/antagonists & inhibitors , Animals , Benzodiazepinones/chemical synthesis , Benzodiazepinones/chemistry , Dogs , Guinea Pigs , Mice , Molecular Structure , Rats , Stereoisomerism , Structure-Activity Relationship , Tissue Distribution
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