Synthesis and SAR of α-sulfonylcarboxylic acids as potent matrix metalloproteinase inhibitors

A series of novel carboxylic acid-based α-sulfone MMP inhibitors have been synthesized and the in vitro enzyme SAR is discussed. A potential binding mode in the active site of the MMP-9 homology model was highlighted. These compounds are potent MMP-9 inhibitors and are selective over MMP-1.

Graphical abstractA series of novel carboxylic acid-based α-sulfone MMP inhibitors have been synthesized and the in vitro enzyme SAR and in vivo PK evaluation are discussed. These compounds are potent MMP-9 inhibitors and are selective over MMP-1.Figure optionsDownload full-size imageDownload as PowerPoint slide