Document Detail


Chiral 1,4-benzodiazepine. VII. Cyclization rates of 2-(n-alpha-ammoniumacyl)-amino-5-chloro-benzophenones in the chiral 1,4-benzodiazepin-2-ones.
MedLine Citation:
PMID:  1174029     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Cyclisation rates of some S-alpha-amino acid derivatives (I--VII) into chiral 1,4-benzodiazepin-2-ones were determined under physiological-like conditions (pH, temperature) and plotted against pKa values of the corresponding alpha-amino acids. No correlation between k, i.e. t1/2 values, of the acidic precursors, and pharmacodynamic activity, as determined by some standard tests, were observed, however. Unambiguity of cyclisation, and its t1/2 values reveal benefit for physico-chemical properties of the investigated acyclic precursors as transport-forms of the chiral 1,4-benzodiazepin-2-ones with prolonged pharmacological activity.
Authors:
V Sunjić; J Kuftinec; F Kajfez
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Arzneimittel-Forschung     Volume:  25     ISSN:  0004-4172     ISO Abbreviation:  Arzneimittelforschung     Publication Date:  1975 Mar 
Date Detail:
Created Date:  1975-11-05     Completed Date:  1975-11-05     Revised Date:  2004-11-17    
Medline Journal Info:
Nlm Unique ID:  0372660     Medline TA:  Arzneimittelforschung     Country:  GERMANY, WEST    
Other Details:
Languages:  eng     Pagination:  340-3     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Aggression / drug effects
Amino Acids
Animals
Behavior, Animal / drug effects
Benzodiazepinones / chemical synthesis*,  pharmacology
Benzophenones
Cyclization
Electroshock
Female
Humans
Kinetics
Lethal Dose 50
Male
Mice
Pentylenetetrazole / antagonists & inhibitors
Seizures / prevention & control
Chemical
Reg. No./Substance:
0/Amino Acids; 0/Benzodiazepinones; 0/Benzophenones; 54-95-5/Pentylenetetrazole

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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