|
|||||
|
|
C-8 Modifications of 3-alkyl-1,8-dibenzylxanthines as inhibitors of human cytosolic phosphoenolpyruvate carboxykinase |
|
| Authors: | Pietranico Sherrie L Foley Louise H Huby Nicholas Yun Weiya Dunten Pete Vermeulen John Wang Ping Toth Katherine Ramsey Gwendolyn Gubler Mary-Lou Wertheimer Stanley J |
| Affiliation: | Department of Discovery Chemistry, Roche Research Center, Hoffmann-La Roche Inc., Nutley, NJ 07110, USA. |
| 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(50) of 0.29+/-0.08 microM. An X-ray analysis of a heteroaromatic sulfonamide is presented showing a new pi-pi interaction. |
| Keywords: | |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |