Pharmacology of some metabolites of triazolam, alprazolam, and diazepam prepared by a simple, one-step oxidation of benzodiazepines.

摘要: A simple, one-step chemical oxidation of triazolam (7) to its 4-hydroxy analogue, 7a, has been developed and applied other triazolo- imidazobenzodiazepines. The reaction may be used convert diazepam temazepam. 4-Hydroxytriazolo[4,3-a][1,4]benzodiazepines have low central nervous system sedative anticonvulsant activity in sharp contrast metabolites which remain active. While 10, an alpha-hydroxy metabolite triazolam, retains much the 7, 10a, alpha,4-dihydroxy is 250 times less potent than 7 on nicotine-antagonism assay over 300 traction assay.