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Sci. Pharm. 2010, 78(2), 155-170; doi:10.3797/scipharm.1004-12

Antidepressant/Anxiolytic and Anti-Nociceptive Effects of Novel 2-Substituted 1,4-Benzodiazepine-2-ones

1
School of Life & Health Sciences, Pharmacy, Aston University, Aston Triangle, Birmingham B4 7ET, England
2
Department of Pharmacology, Faculty of Medicine, Khon Kaen University, 40002 Khon Kaen, Thailand
*
Author to whom correspondence should be addressed.
Received: 15 April 2010 / Accepted: 17 May 2010 / Published: 17 May 2010
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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.
Keywords: Oxazepam; 2-Substituted 1,4-benzodiazepine; Analgesics; Antidepressants; In vivo studies; Dye Oxazepam; 2-Substituted 1,4-benzodiazepine; Analgesics; Antidepressants; In vivo studies; Dye
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

SINGH, H.; SATTAYASAI, J.; LATTMANN, P.; BOONPRAKOB, Y.; LATTMANN, E. Antidepressant/Anxiolytic and Anti-Nociceptive Effects of Novel 2-Substituted 1,4-Benzodiazepine-2-ones. Sci. Pharm. 2010, 78, 155-170.

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