Chiral 1,4-benzodiazepine. VII. Cyclization rates of 2-(n-alpha-ammoniumacyl)-amino-5-chloro-benzophenones in the chiral 1,4-benzodiazepin-2-ones.
Arzneimittelforschung
; 25(3): 340-3, 1975 Mar.
Article
em En
| MEDLINE
| ID: mdl-1174029
ABSTRACT
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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Base de dados:
MEDLINE
Assunto principal:
Benzodiazepinonas
Limite:
Animals
/
Female
/
Humans
/
Male
Idioma:
En
Ano de publicação:
1975
Tipo de documento:
Article