5-Chloroindoloyl glycine amide inhibitors of glycogen phosphorylase: synthesis, in vitro, in vivo, and X-ray crystallographic characterization

…, VL Rath, PE Genereux, DL Hageman, CB Levy…

文献索引：Wright, Stephen W.; Rath, Virginia L.; Genereux, Paul E.; Hageman, David L.; Levy, Carolyn B.; McClure, Lester D.; McCoid, Scott C.; McPherson, R. Kirk; Schelhorn, Teresa M.; Wilder, Donald E.; Zavadoski, William J.; Gibbs, E. Michael; Treadway, Judith L. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 2 p. 459 - 465

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被引用次数: 29

摘要

The synthesis, in vitro, and in vivo biological characterization of a series of achiral 5- chloroindoloyl glycine amide inhibitors of human liver glycogen phosphorylase A are described. Improved potency over previously reported compounds in cellular and in vivo assays was observed. The allosteric binding site of these compounds was shown by X-ray crystallography to be the same as that reported previously for 5-chloroindoloyl norstatine ...