کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10588268 | 981450 | 2011 | 17 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and structure-activity relationship of new 1,5-dialkyl-1,5-benzodiazepines as cholecystokinin-2 receptor antagonists
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله

چکیده انگلیسی
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.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 14, 15 July 2011, Pages 4257-4273
Journal: Bioorganic & Medicinal Chemistry - Volume 19, Issue 14, 15 July 2011, Pages 4257-4273
نویسندگان
Karen Roberts, Antonella Ursini, Robert Barnaby, Paolo G. Cassarà , Mauro Corsi, Giovanni Curotto, Daniele Donati, Aldo Feriani, Gabriella Finizia, Carla Marchioro, Daniela Niccolai, Beatrice Oliosi, Stefano Polinelli, Emiliangelo Ratti, Angelo Reggiani,