title: Antidepressant/anxiolytic and anti-nociceptive effects of novel 2-substituted 1,4-benzodiazepine-2-ones.
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 5aâ5i 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 5â50 mg/kg an analgesic effect in mice.
authors.affiliation: School of Life & Health Sciences, Pharmacy, Aston University, Aston Triangle, Birmingham B4 7ET, England.
authors.forename: Harjit
authors.initials: H
authors.lastname: Singh
authors.forename: Jintana
authors.initials: J
authors.lastname: Sattayasai
authors.forename: Pornthip
authors.initials: P
authors.lastname: Lattmann
authors.forename: Yodchai
authors.initials: Y
authors.lastname: Boonprakob
authors.forename: Eric
authors.initials: E
authors.lastname: Lattmann