1227191-49-2Relevant academic research and scientific papers
HETEROARYL DIAMIDE COMPOUNDS USEFUL AS MMP-13 INHIBITORS
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Page/Page column 93, (2010/06/15)
Disclosed are compounds and compositions of the formula (I) as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula (I).
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.
