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Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines.

Authors :
Gall M
Kamdar BV
Collins RJ
Source :
Journal of medicinal chemistry [J Med Chem] 1978 Dec; Vol. 21 (12), pp. 1290-4.
Publication Year :
1978

Abstract

A simple, one-step chemical oxidation of triazolam (7) to its 4-hydroxy analogue, 7a, has been developed and applied to other triazolo- and imidazobenzodiazepines. The reaction may be used to convert diazepam to temazepam. 4-Hydroxytriazolo[4,3-a][1,4]benzodiazepines have low central nervous system sedative and anticonvulsant activity in sharp contrast to metabolites of diazepam which remain active. While 10, an alpha-hydroxy metabolite of triazolam, retains much of the activity of 7, 10a, and alpha,4-dihydroxy metabolite of triazolam, is 250 times less potent than 7 on the nicotine-antagonism assay and over 300 times less potent on the traction assay.

Details

Language :
English
ISSN :
0022-2623
Volume :
21
Issue :
12
Database :
MEDLINE
Journal :
Journal of medicinal chemistry
Publication Type :
Academic Journal
Accession number :
31483
Full Text :
https://doi.org/10.1021/jm00210a022