| 17513107 |
More SS, Vince R: Design, synthesis, and binding studies of bidentate Zn-chelating peptidic inhibitors of glyoxalase-I. Bioorg Med Chem Lett. 2007 Jul 1;17(13):3793-7. Epub 2006 Dec 21.
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. |
32(0,1,1,2) |