SYNTHESIS OF SUBSTRATE-ANALOGS AND INHIBITORS FOR THE PHOSPHOGLYCERATE MUTASE ENZYME

Several substrate analogues of the title enzyme were synthesized as we ll as with possible irreversible inhibitors, analogues of phosphoglyco late, the cofactor for this enzyme. The main routes involved an Arbuzo v type reaction on functionalized halides, a reaction significantly im proved by a sonication procedure and reaction of the diethylphosphite anion on tosylates. Phosphorylated epoxides were obtained by quantitat ive oxidation of conjugate double bonds using DMDO. Preliminary assays indicated a promising activity in some of these compounds.