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Benzisothiazolyliminothiazolidin‐4‐ones with Chondroprotective Properties: Searching for Potent and Selective Inhibitors of MMP‐13
Author(s) -
Vicini Paola,
Crascì Lucia,
Incerti Matteo,
Ronsisvalle Simone,
Cardile Venera,
Panico Anna Maria
Publication year - 2011
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201100223
Subject(s) - matrix metalloproteinase , allosteric regulation , chemistry , chelation , matrix metalloproteinase inhibitor , combinatorial chemistry , scaffold , molecular model , matrix (chemical analysis) , stereochemistry , enzyme , computational biology , biochemistry , biology , medicine , organic chemistry , biomedical engineering , chromatography
Caring for cartilage: A potent and selective matrix metalloproteinase‐13 (MMP‐13) inhibitor has been discovered with a novel 2‐benzisothiazolylimino‐5‐benzylidenethiazolidin‐4‐one scaffold. The structure–activity relationships of the three positional methoxybenzylidene isomers with respect to their chondroprotective effects was evaluated. Molecular modeling provided insight into the binding mode of these non‐zinc‐chelating (allosteric) inhibitors with MMP‐13.