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

Harjit Singh, Jintana Sattayasai, Pornthip Lattmann, Yodchai Boonprakob, Eric Lattmann*

*Corresponding author for this work

Research output: Contribution to journalArticle

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.

Original languageEnglish
Pages (from-to)155-169
Number of pages15
JournalScientia Pharmaceutica
Volume78
Issue number2
DOIs
Publication statusPublished - 17 May 2010

Bibliographical note

© 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.

Keywords

  • 2-Substituted 1
  • 4-Benzodiazepine
  • analgesics
  • antidepressants
  • dye
  • in vivo studies
  • Oxazepam

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