γ-L-Glutamyl-O-acyl-L-serylglycine derivatives: synthesis, purification and evaluation as inhibitors of glyoxalases

Abstract

Oxygen ester analogues of S-D-lactoylglutathione, γ-L-glutamyl-O-acyl-L-serylglycine derivatives, were synthesised and evaluated as inhibitors of glyoxalase II. They were competitive inhibitors where the inhibition constant K_i, decreased with increase in acyl chain length. γ-L-Glutamyl-O-acyl-L-serylglycine derivatives also inhibit glyoxalase I. These compounds provide a novel route to glyoxalase II inhibitors for cancer chemotherapy.