SAR studies of non-zinc-chelating MMP-13 inhibitors: Improving selectivity and metabolic stability

SAR studies to improve the selectivity and metabolic stability of a class of recently discovered MMP-13 inhibitors are reported. Improved selectivity was achieved by modifying interactions with the S1′ pocket. Metabolic stability was improved through reduction of inhibitor lipophilicity. This translated into lower in vivo clearance for the preferred compound.

SAR studies to improve the selectivity and metabolic stability of a class of recently discovered non-Zn-chelating MMP-13 inhibitors are reported.Figure optionsDownload as PowerPoint slide