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  • Title: Amino acid anthranilamide derivatives as a new class of glycogen phosphorylase inhibitors.
    Author: Evans KA, Li YH, Coppo FT, Graybill TL, Cichy-Knight M, Patel M, Gale J, Li H, Thrall SH, Tew D, Tavares F, Thomson SA, Weiel JE, Boucheron JA, Clancy DC, Epperly AH, Golden PL.
    Journal: Bioorg Med Chem Lett; 2008 Jul 15; 18(14):4068-71. PubMed ID: 18554908.
    Abstract:
    A series of amino acid anthranilamide derivatives identified from a high-throughput screening campaign as novel, potent, and glucose-sensitive inhibitors of human liver glycogen phosphorylase a are described. A solid-phase synthesis using Wang resin was also developed which provided efficient access to a variety of analogues, and resulted in the identification of key structure-activity relationships, and the discovery of a potent exemplar (IC(50)=80 nM). The SAR scope, synthetic strategy, and in vitro results for this series are presented herein.
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