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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
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Author to whom correspondence should be addressed.
Sci. Pharm. 2010, 78(2), 155-170; https://doi.org/10.3797/scipharm.1004-12
Received: 15 April 2010 / Accepted: 17 May 2010 / Published: 17 May 2010
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
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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