| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10595177 | Bioorganic & Medicinal Chemistry Letters | 2012 | 4 Pages |
Abstract
AX10185, the phenyl amide of xanthurenic acid, was found to be a sub-100Â nM inhibitor of Lp-PLA2. However, in the presence of EDTA the inhibitory activity of AX10185 was extinguished while the enzymatic activity of Lp-PLA2 did not change. Subsequent metal screening experiments determined the inhibition to be Zn2+ dependent. Structure-activity relationship studies indicated the presence of the 4-hydroxy group to be critical and selected substituted phenyl, polycyclic, and cycloaliphatic amides of xanthurenic acid to be well tolerated.
Keywords
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Emme C.K. Lin, Yi Hu, Christopher M. Amantea, Lan M. Pham, Julia Cajica, Eric Okerberg, Heidi E. Brown, Allister Fraser, Lingling Du, Yasushi Kohno, Junichi Ishiyama, John W. Kozarich, Kevin R. Shreder,