Author/Authors :
Sherrie L. Pietranico، نويسنده , , Louise H. Foley، نويسنده , , Nicholas Huby، نويسنده , , Weiya Yun، نويسنده , , Pete Dunten، نويسنده , , John Vermeulen، نويسنده , , Ping Wang، نويسنده , , Katherine Toth، نويسنده , , Gwendolyn Ramsey، نويسنده , , Mary-Lou Gubler، نويسنده , , Stanley J. Wertheimer، نويسنده ,
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 IC50 of 0.29 ± 0.08 μM. An X-ray analysis of a heteroaromatic sulfonamide is presented showing a new π–π interaction.
Keywords :
Enzyme and cellular assays , cPEPCK inhibitors , x-ray , Xanthine class
