| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10588052 | Bioorganic & Medicinal Chemistry Letters | 2013 | 4 Pages |
Abstract
AX10479, the phenyl amide of 4-hydroxy-8-methanesulfonylamino-quinoline-2-carboxylic acid, was identified as a Zn2+-dependent, 27Â nM inhibitor of human plasma Lp-PLA2. Structure-activity relationship studies focused on the AX10479 2-phenylamide group identified equipotent cycloaliphatic amides, an enantioselective preference for chiral amides, and phenyl substitution patterns (e.g., 2-methyl-3-fluoro) that increased potency.
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Authors
Yi Hu, Emme C.K. Lin, Lan M. Pham, Julia Cajica, Christopher M. Amantea, Eric Okerberg, Heidi E. Brown, Allister Fraser, Lingling Du, Yasushi Kohno, Junichi Ishiyama, John W. Kozarich, Kevin R. Shreder,