Design & Synthesis of some new 6-hydrox-yperhydro-1,4-diazepine-2,3-dione derivatives of potential Biological Activity

Faculty Pharmacy Year: 2005
Type of Publication: Theses Pages: 150
Authors:
BibID 3211487
Keywords : Organic compounds    
Abstract:
6-Hydroxyperhydro-1,4-Diazepine-2,3-Dione Derivatives-Design and SynthesisThe 1,4-diazepine ring is embedded in the structure of benzodiazepines which constitute the most widely prescribed class of compounds in current clinical use . In view of SAR and mode of action of benzodiazepines , it is clear that the benzene ring ( ring A; skeleton XX111 ) plays a crucial role in the activity of these compounds as CNS depressants , since it binds with the lipophilic area ( L2 ) of the BZS receptor .Replacement of ring A by other heterocyclic rings as in comounds V , XVI , XXIV , and XXVII retained most of the CNS depressant activities of the parent benzodiazepines with increased toxicity . Moreover , inspection of the review of literatures of 1,4-dizepines where the benzene ring A was dwleted resulted in compounds lacking the CNS depressant activity but having other activities such as :A - Antiemtic ; compound ( XXXIII ) .B - Neurotropic ; compounds ( XXXIV ) and XXXV ) .C - CNS cholinergic compounds including those for treatment of neurodegenerative diseases ; compound ( XXXVI ) .D - Analgesic anti-inflammatory ; ( XXXVII ) . 
   
     
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