| 19969459 |
Jerome KD, Rucker PV, Xing L, Shieh HS, Baldus JE, Selness SR, Letavic MA, Braganza JF, McClure KF: Continued exploration of the triazolopyridine scaffold as a platform for p38 MAP kinase inhibition. Bioorg Med Chem Lett. 2010 Jan 15;20(2):469-73. Epub 2009 Nov 26.
The structure based drug design, synthesis and structure-activity relationship of a series of C6 sulfur linked triazolopyridine based p38 inhibitors are described. The metabolic deficiencies of this series were overcome through changes in the C6 linker from sulfur to methylene, which was predicted by molecular modeling to be bioisosteric. X-ray of the ethylene linked compound 61 confirmed the predicted binding orientation of the scaffold in the p38 enzyme. |
32(0,1,1,2) |