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Synthesis and structure-activity relationship of new 1,5-dialkyl-1,5-benzodiazepines as cholecystokinin-2 receptor antagonists.

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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

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

doi

10.1016/j.bmc.2011.05.057

subject

Has Abstract

pub_date

2011-07-15 00:00:00

pages

4257-73

issue

14

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(11)00420-2

journal_volume

19

pub_type

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