Inhibition of acetylcholinesterase by new physostigmine derivatives

The kinetics of inhibition of acetylcholinesterase (AChE, EC 3.1.1.7) from electric eel by new physostigmine derivatives in which the methylcarbamic group has been substituted with monoalkylcarbamic, dialkylcarbamic and phenylcarbamic groups was studied. The new compounds are competitive inhibitors of AChE and show a lower anticholinesterase activity than physostigmine. The anticholinesterase activity, the bimolecular rate constant ki and the carbamylation constant k2 have been measured for some selected derivatives.