Design and Synthesis of 1,3-Disubstitiuted-2-Pyridones as a New Class of Glycogen Phosphorylase Inhibitors

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Author(s)
Primary Supervisor
Jenkins, Ian
Loughlin, Wendy
Year published
2009
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Glycogen Phosphorylase (GP) is the regulatory enzyme that catalyses the first step in glycogen degradation and is a potential enzyme target for therapeutic intervention in the treatment of diabetes. The 16 amino acid C-terminal sequence of human Gl is the only known targeting subunit that binds to GPa. Blocking the interactions between Gl and GPa should reduce high blood glucose levels in a diabetic person. A segment of the 16 amino acid segment was chosen for a small molecule peptidomimetric approach, and de nova design from this segment identified the pyridone ring as apotential scaffold. This thesis reports the design and ...
View more >Glycogen Phosphorylase (GP) is the regulatory enzyme that catalyses the first step in glycogen degradation and is a potential enzyme target for therapeutic intervention in the treatment of diabetes. The 16 amino acid C-terminal sequence of human Gl is the only known targeting subunit that binds to GPa. Blocking the interactions between Gl and GPa should reduce high blood glucose levels in a diabetic person. A segment of the 16 amino acid segment was chosen for a small molecule peptidomimetric approach, and de nova design from this segment identified the pyridone ring as apotential scaffold. This thesis reports the design and synthesis of 1.3-disubstituted pyridones as new class of GPa inhibitors.
View less >
View more >Glycogen Phosphorylase (GP) is the regulatory enzyme that catalyses the first step in glycogen degradation and is a potential enzyme target for therapeutic intervention in the treatment of diabetes. The 16 amino acid C-terminal sequence of human Gl is the only known targeting subunit that binds to GPa. Blocking the interactions between Gl and GPa should reduce high blood glucose levels in a diabetic person. A segment of the 16 amino acid segment was chosen for a small molecule peptidomimetric approach, and de nova design from this segment identified the pyridone ring as apotential scaffold. This thesis reports the design and synthesis of 1.3-disubstituted pyridones as new class of GPa inhibitors.
View less >
Thesis Type
Thesis (PhD Doctorate)
Degree Program
Doctor of Philosophy (PhD)
School
Eskitis Institute for Cell and Molecular Therapies
Copyright Statement
The author owns the copyright in this thesis, unless stated otherwise.
Item Access Status
Public
Note
This thesi was scanned.
The appendix and published articles have not been published.
Subject
Glycogen phosphorylase inhibitors
Glycogen phosphorylase
Glycogen degradation
pyridone analogues
Pyridones