The synthesis and in vitro acetylcholinesterase and butyrylcholinesterase inhibitory activity of tacrine (Cognex®) derivaties

Abstract Chlorosubstituted derivatives of tacrine ( 1 ), 1,4-methylenetacrine ( 2 , and their in vitro acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities are described. The most potent analogues are 6-chlorotacrine ( 1b ) in AChE and 7-chlorotacrine ( 1c ) in BChE inhibition.