Novel 3,4-dihydroquinolin-2(1H)-one inhibitors of human glycogen phosphorylase a

Bioorg Med Chem Lett. 2003 Dec 15;13(24):4385-8. doi: 10.1016/j.bmcl.2003.09.022.

Abstract

The preparation of a series of substituted indoles coupled to six- and seven-membered cyclic lactams is described and their role as human glycogen phosphorylase a inhibitors discussed. The SAR of the indole moiety and lactam ring are presented.

MeSH terms

  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Glycogen Phosphorylase / antagonists & inhibitors*
  • Humans
  • Kinetics
  • Models, Molecular
  • Molecular Conformation
  • Quinolines / chemical synthesis*
  • Quinolines / chemistry
  • Quinolines / pharmacology*
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Quinolines
  • Glycogen Phosphorylase