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

@article{Gao2010SARSO,
  title={SAR studies of non-zinc-chelating MMP-13 inhibitors: improving selectivity and metabolic stability.},
  author={Donghong Amy Gao and Zhaoming Xiong and Alexander Heim-Riether and Laura M Amodeo and E Michael August and Xianhua Cao and Leonard Ciccarelli and Brandon K Collins and Kyle Harrington and Kathleen Haverty and Melissa Hill-Drzewi and Xiang Li and Shuang Liang and Steluta Mariana Margarit and Neil Moss and Nelamangala V Nagaraja and J. Proudfoot and Rene Roman and Sabine Schlyer and Lana Smith Keenan and Steven J Taylor and Bernd Wellenzohn and Dieter Wiedenmayer and Jun Li and Neil A. Farrow},
  journal={Bioorganic & medicinal chemistry letters},
  year={2010},
  volume={20 17},
  pages={5039-43}
}
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. 

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