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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.
Bioorg Med Chem Lett ; 20(17): 5039-43, 2010 Sep 01.
Article in English | MEDLINE | ID: mdl-20675133

ABSTRACT

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.


Subject(s)
Matrix Metalloproteinase Inhibitors , Protease Inhibitors/chemistry , Protease Inhibitors/pharmacology , Chelating Agents/chemistry , Chelating Agents/pharmacology , Structure-Activity Relationship , Zinc/chemistry
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