Synthesis and Biological Activity of (Z)-Dialkylaminoalkylamides of N-Benzoyl-α,β-Dehydroamino Acids and Their Iodomethylates

A series of N , N -(dialkylamino)alkylamides of several N -substituted α,β-dehydroamino acids and their quaternary ammonium salts were synthesized via the reaction of unsaturated 5(4 H )-oxazolones with N , N -dialkyldiamines and characterized by physicochemical characteristics. Their reactions with human erythrocytic acetylcholinesterase (ACE) and plasmic butyrylcholinesterase (BuCE) were studied. The IC 50 values [concentration at which the hydrolysis rate of cholinesterase was 50% inhibited by acetylthiocholine (0.1 mM)] of all synthesized compounds were determined. It was found that all synthesized compounds possessed anticholinesterase activity and were specific mainly for BuCE.