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ID: ALA1146153

Journal: Bioorg Med Chem Lett

Title: A metabolically stable tight-binding transition-state inhibitor of glyoxalase-I.

Authors: More SS, Vince R.

Abstract: The design, synthesis, and enzyme kinetics evaluation of a transition-state inhibitor of glyoxalase-I is described. The union of the hydroxamic acid zinc-chelator with a urea isostere for the glu-cys amide bond led to a glutathione analog which retained inhibitory potency toward glyoxalase-I while possessing resistance toward gamma-glutamyltranspeptidase mediated breakdown. This compound is viewed as a potential lead for the development of second-generation glyoxalase-I inhibitors wherein, the problems pertaining to metabolism and selectivity are overcome.

CiteXplore: 16997560

DOI: 10.1016/j.bmcl.2006.08.121