409107-69-3Relevant academic research and scientific papers
Sultam hydroxamates as novel matrix metalloproteinase inhibitors
Cherney, Robert J.,Mo, Ruowei,Meyer, Dayton T.,Hardman, Karl D.,Liu, Rui-Qin,Covington, Maryanne B.,Qian, Mingxin,Wasserman, Zelda R.,Christ, David D.,Trzaskos, James M.,Newton, Robert C.,Decicco, Carl P.
, p. 2981 - 2983 (2007/10/03)
In this communication we describe the design, synthesis, and evaluation of novel sultam hydroxamates 4 as MMP-2, -9, and -13 inhibitors. Compound 26 was found to be an active inhibitor (MMP-2 IC50 = 1 nM) with 1000-fold selectivity over MMP-1 and good oral bioavailability (F = 43%) in mouse. An X-ray crystal structure of 26 in MMP-13 confirms the key hydrogen bonds and prime side binding in the active site.
