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ID: ALA1139998

Journal: Bioorg Med Chem Lett

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

Authors: More SS, Vince R.

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 the resultant beta-keto ester compounds are reported.

CiteXplore: 17513107

DOI: 10.1016/j.bmcl.2006.12.056