1227191-22-1Relevant articles and documents
SAR studies of non-zinc-chelating MMP-13 inhibitors: Improving selectivity and metabolic stability
Gao, Donghong Amy,Xiong, Zhaoming,Heim-Riether, Alexander,Amodeo, Laura,August, E. Michael,Cao, Xianhua,Ciccarelli, Leonard,Collins, Brandon K.,Harrington, Kyle,Haverty, Kathleen,Hill-Drzewi, Melissa,Li, Xiang,Liang, Shuang,Margarit, Steluta Mariana,Moss, Neil,Nagaraja, Nelamangala,Proudfoot, John,Roman, Rene,Schlyer, Sabine,Keenan, Lana Smith,Taylor, Steven,Wellenzohn, Bernd,Wiedenmayer, Dieter,Li, Jun,Farrow, Neil A.
scheme or table, p. 5039 - 5043 (2010/10/18)
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.
