Antidepressant/anxiolytic and anti-nociceptive effects of novel 2-substituted 1,4-benzodiazepine-2-ones

Singh, Harjit, Sattayasai, Jintana, Lattmann, Pornthip, Boonprakob, Yodchai and Lattmann, Eric (2010). Antidepressant/anxiolytic and anti-nociceptive effects of novel 2-substituted 1,4-benzodiazepine-2-ones. Scientia Pharmaceutica, 78 (2), pp. 155-169.

Abstract

Oxazepam (4a) has been used as overall starting material in the synthesis of novel 2-substituted 1,4-benzodiazepines. By reacting Oxazepam 4a with commercially available hydrazines, hydrazides, semicarbazide, aminoguanidine and N,N-dimethylamino aniline in ethanol under acetic conditions, a series of diazenyl-1,4-benzodiazepines 5a-5i and 2-amino- 1,4-benzodiazepine 5k were obtained in good yields. These novel compounds served as new chemical entities (NCE) for testing in mice. The diazo-benzodiazepine 5d has shown a promising antidepressant effect in initial experiments in vivo at a dose of 5 mg/kg. The highly coloured 2-aminobenzodiazepine derivative 5k showed over a dose range from 5-50 mg/kg an analgesic effect in mice.

Publication DOI: https://doi.org/10.3797/scipharm.1004-12
Divisions: Life & Health Sciences > Pharmacy
Life & Health Sciences
Additional Information: © Singh et al.; licensee Österreichische Apotheker-Verlagsgesellschaft m. b. H., Vienna, Austria. This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by /3.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
Uncontrolled Keywords: 2-Substituted 1,4-Benzodiazepine,analgesics,antidepressants,dye,in vivo studies,Oxazepam,Pharmaceutical Science
Full Text Link: http://www.scip ... sp?id=646&lid=2
Related URLs: http://www.scop ... tnerID=8YFLogxK (Scopus URL)
Published Date: 2010-05-17
Authors: Singh, Harjit
Sattayasai, Jintana
Lattmann, Pornthip
Boonprakob, Yodchai
Lattmann, Eric

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