Bioorganic & medicinal chemistry letters

Design, synthesis, and binding studies of bidentate Zn-chelating peptidic inhibitors of glyoxalase-I

SS More, R Vince

Index: More, Swati S.; Vince, Robert Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 13 p. 3793 - 3797

Full Text: HTML

Citation Number: 9

Abstract

The known affinity of ethyl acetoacetate (ACC) toward divalent zinc prompted us to attempt its employment as a chelating moiety in the design of glyoxalase-I inhibitors. A practical synthetic route was developed to incorporate this pharmacophore into the side chain of glutamic acid, with flexibility to allow incorporation of additional functionality at the end-stage of the synthesis. Herein, the details of this synthetic approach as well as the evaluation of ...