SYNTHESES AND ANTICHOLINESTERASE ACTIVITY OF TETRAHYDROBENZAZEPINE CARBAMATES

The synthesis of a series of alkylcarbamates of ,5-methano-2,3,4,5-tet rahydro-1H-2-benzazepin-7-ol is reported. Many of these compounds are potent acetylcholinesterase (AChE) inhibitors. The in vitro AChE inhib ition, cholinergic effects, acute toxicity, and elevation of brain ace tylcholine levels in vivo of this series of compounds are described, A representative compound, 1d (5,6 mg/kg, po), was able to reverse hemi colinium-3-induced amnesia in the mouse passive avoidance assay.