Synthesis and pharmacology of novel anxiolytic agents derived from 2-[(dialkylamino)methyl-4H-triazol-4-yl] benzophenones and related heterocyclic benzophenones.

摘要: A series of novel [(dialkylamino)methyl-4H-1,2,4-triazol-4-yl]benzophenones and related compounds has been prepared via total synthesis from substituted aminodiphenylmethanes or by hydrolysis subsequent methylation triazolobenzodiazepines. These new triazole were found to have potent sedative muscle relaxing activity in mice (i.e., these depressed the traction dish reflexes). In addition, title antagonized clonic convulsions induced administration pentylenetratrazole (Metrazol, 85 mg/kg), with ED50's varying 2.0 23.0 mg/kg, lethality thiosemicarbazide, 0.02 9.0 mg/kg. several biological tests, potency seven benzophenone derivatives approached exceed that diazepam (35a) its glycylaminobenzophenone analogue 36.