1. C-8 Modifications of 3-alkyl-1,8-dibenzylxanthines as inhibitors of human cytosolic phosphoenolpyruvate carboxykinase
- Author
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Sherrie L. Pietranico, Ping Wang, Nicholas John Silvester Huby, Mary-Lou Gubler, Louise H. Foley, Weiya Yun, John Vermeulen, Stanley Wertheimer, Gwendolyn Ramsey, Pete William Dunten, and Katherine Toth
- Subjects
chemistry.chemical_classification ,Models, Molecular ,Bicyclic molecule ,Stereochemistry ,Organic Chemistry ,Clinical Biochemistry ,Pharmaceutical Science ,Lyase ,Biochemistry ,Chemical synthesis ,Sulfonamide ,chemistry.chemical_compound ,Cytosol ,chemistry ,Amide ,Xanthines ,Drug Discovery ,Molecular Medicine ,Humans ,Phosphoenolpyruvate Carboxykinase (GTP) ,Enzyme Inhibitors ,Phosphoenolpyruvate carboxykinase ,Molecular Biology ,Derivative (chemistry) ,Alkyl - Abstract
New modifications on the C-8 4-aminobenzyl unit of the previously reported 3-alkyl-1,8-dibenzylxanthine inhibitors of cPEPCK are presented. The most active compound reported here is the 5-chloro-1,3-dimethyl-1H-pyrazole-4-sulfonic acid amide derivative 2 with an IC{sub 50} of 0.29 {+-} 0.08 {mu}M. An X-ray analysis of a heteroaromatic sulfonamide is presented showing a new {pi}-{pi} interaction.
- Published
- 2007