2. Academic Validation
  3. 5-Chloroindoloyl glycine amide inhibitors of glycogen phosphorylase: synthesis, in vitro, in vivo, and X-ray crystallographic characterization

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

  • Bioorg Med Chem Lett. 2005 Jan 17;15(2):459-65. doi: 10.1016/j.bmcl.2004.10.048.
Stephen W Wright 1,  Virginia L Rath,  Paul E Genereux,  David L Hageman,  Carolyn B Levy,  Lester D McClure,  Scott C McCoid,  R Kirk McPherson,  Teresa M Schelhorn,  Donald E Wilder,  William J Zavadoski,  E Michael Gibbs,  Judith L Treadway
Affiliations

Affiliation

  • 1 Pfizer Global Research and Development, Eastern Point Road, Groton, CT 06340, USA. [email protected]
PMID: 15603973 DOI: 10.1016/j.bmcl.2004.10.048
Abstract

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 amides.

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