| Literature DB >> 15163180 |
Robert J Cherney1, Ruowei Mo, Dayton T Meyer, Karl D Hardman, Rui-Qin Liu, Maryanne B Covington, Mingxin Qian, Zelda R Wasserman, David D Christ, James M Trzaskos, Robert C Newton, Carl P Decicco.
Abstract
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 IC(50) = 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.Entities:
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Year: 2004 PMID： 15163180 DOI： 10.1021/jm049833g
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446