Synthesis and structure-activity relationship of new 1,5-dialkyl-1,5-benzodiazepines as cholecystokinin-2 receptor antagonists |
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Authors: | Roberts Karen Ursini Antonella Barnaby Robert Cassarà Paolo G Corsi Mauro Curotto Giovanni Donati Daniele Feriani Aldo Finizia Gabriella Marchioro Carla Niccolai Daniela Oliosi Beatrice Polinelli Stefano Ratti Emiliangelo Reggiani Angelo Tedesco Giovanna Tranquillini Maria E Trist David G van Amsterdam Franciscus T M |
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Affiliation: | GlaxoSmithKline, Medicines Research Centre, Via A. Fleming, 4, 37100 Verona, Italy. karen.l.roberts@gsk.com |
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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. |
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