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  • Title: Synthesis and structure-activity relationships of 3-phenyl-2-propenamides as inhibitors of glycogen phosphorylase a.
    Author: Li YH, Coppo FT, Evans KA, Graybill TL, Patel M, Gale J, Li H, Tavares F, Thomson SA.
    Journal: Bioorg Med Chem Lett; 2006 Nov 15; 16(22):5892-6. PubMed ID: 16942879.
    Abstract:
    A series of 3-phenyl-2-propenamides discovered from a high-throughput screening campaign as novel, potent, glucose-sensitive inhibitors of human liver glycogen phosphorylase a is described. A solid-phase synthesis on DMHB resin was also developed which provided efficient access not only to certain analogues that could not be cleanly made using more traditional means, but also to a variety of additional analogues. The SAR scope and synthetic strategy are presented herein.
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