| Literature DB >> 20675133 |
Donghong Amy Gao1, Zhaoming Xiong, Alexander Heim-Riether, Laura Amodeo, E Michael August, Xianhua Cao, Leonard Ciccarelli, Brandon K Collins, Kyle Harrington, Kathleen Haverty, Melissa Hill-Drzewi, Xiang Li, Shuang Liang, Steluta Mariana Margarit, Neil Moss, Nelamangala Nagaraja, John Proudfoot, Rene Roman, Sabine Schlyer, Lana Smith Keenan, Steven Taylor, Bernd Wellenzohn, Dieter Wiedenmayer, Jun Li, Neil A Farrow.
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. Copyright 2010 Elsevier Ltd. All rights reserved.Mesh：
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Year: 2010 PMID： 20675133 DOI： 10.1016/j.bmcl.2010.07.036
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823