A CONVENIENT METHOD FOR THE SYNTHESIS OF PHOSPHOROTHIOATES AND THEIR ANTICHOLINESTERASE ACTIVITIES

Abstract

A simple, efficient, and general method has been developed for the synthesis of phosphorothioates through a one-pot reaction of alkyl halides with the mixture of diethyl phosphite in the presence of NH ₄ OAc/S/CaO under solvent–free conditions. The anticholinesterase activities of eight different phosphorothioates were investigated on acetylcholinesterase from electric eel.

Keywords:

• Ammonium acetate
• anticholinesterase activity
• calcium oxide
• phosphorothioate
• sulfur

We thank the Institute for Advanced Studies in Basic Sciences for supporting this work. We are also grateful to Dr. E. Shams for helpful discussion and Mr. K. Navaee for technical assistance.

Notes

^a Isolated yields.

^a The activities were compared to the activity of a control and expressed as percent inhibition.

^b Results shown are averages of triplicate experiments.