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ID: ALA1806366
Journal: Bioorg Med Chem
Title: Synthesis and structure-activity relationship of new 1,5-dialkyl-1,5-benzodiazepines as cholecystokinin-2 receptor antagonists.
Authors: Roberts K, Ursini A, Barnaby R, Cassarà PG, Corsi M, Curotto G, Donati D, Feriani A, Finizia G, Marchioro C, Niccolai D, Oliosi B, Polinelli S, Ratti E, Reggiani A, Tedesco G, Tranquillini ME, Trist DG, van Amsterdam FT.
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.
CiteXplore: 21689940