| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374617 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
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.
Graphical abstractSAR studies to improve the selectivity and metabolic stability of a class of recently discovered non-Zn-chelating MMP-13 inhibitors are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Donghong Amy Gao, 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,