| Literature DB >> 23333209 |
Yi Hu1, 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.
Abstract
AX10479, the phenyl amide of 4-hydroxy-8-methanesulfonylamino-quinoline-2-carboxylic acid, was identified as a Zn(2+)-dependent, 27nM inhibitor of human plasma Lp-PLA(2). 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.Entities:
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Year: 2012 PMID： 23333209 DOI： 10.1016/j.bmcl.2012.11.048
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823