| Chiral 1,4-benzodiazepine. VII. Cyclization rates of 2-(n-alpha-ammoniumacyl)-amino-5-chloro-benzophenones in the chiral 1,4-benzodiazepin-2-ones. | |
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MedLine Citation:
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PMID: 1174029 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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V Sunjić; J Kuftinec; F Kajfez |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Arzneimittel-Forschung Volume: 25 ISSN: 0004-4172 ISO Abbreviation: Arzneimittelforschung Publication Date: 1975 Mar |
Date Detail:
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Created Date: 1975-11-05 Completed Date: 1975-11-05 Revised Date: 2004-11-17 |
Medline Journal Info:
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Nlm Unique ID: 0372660 Medline TA: Arzneimittelforschung Country: GERMANY, WEST |
Other Details:
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Languages: eng Pagination: 340-3 Citation Subset: IM |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Aggression
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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:
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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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