Title of article :
Modified 3-Alkyl-1,8-dibenzylxanthines as GTP-Competitive inhibitors of phosphoenolpyruvate carboxykinase
Author/Authors :
Louise H. Foley، نويسنده , , Ping Wang، نويسنده , , Pete Dunten، نويسنده , , Gwendolyn Ramsey، نويسنده , , Mary-Lou Gubler، نويسنده , , Stanley J. Wertheimer، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2003
Pages :
4
From page :
3607
To page :
3610
Abstract :
The first non-substrate like inhibitors of human cytosolic phosphoenolpyruvate carboxykinase (PEPCK) competitive with GTP are reported. An effort to discover orally active compounds that improve glucose homeostasis in Type 2 diabetics by reversibly inhibiting PEPCK led to the discovery of 1-allyl-3-butyl-8-methylxanthine (5). We now report modifications at N-1 and C-8 that improved the in vitro activity of the initial xanthine HTS hit by 100-fold and a developing SAR for this class of inhibitor.
Journal title :
Bioorganic & Medicinal Chemistry Letters
Serial Year :
2003
Journal title :
Bioorganic & Medicinal Chemistry Letters
Record number :
793620
Link To Document :
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