1424728-22-2Relevant academic research and scientific papers
Amides of 4-hydroxy-8-methanesulfonylamino-quinoline-2-carboxylic acid as zinc-dependent inhibitors of Lp-PLA2
Hu, Yi,Lin, Emme C.K.,Pham, Lan M.,Cajica, Julia,Amantea, Christopher M.,Okerberg, Eric,Brown, Heidi E.,Fraser, Allister,Du, Lingling,Kohno, Yasushi,Ishiyama, Junichi,Kozarich, John W.,Shreder, Kevin R.
, p. 1553 - 1556 (2013/03/14)
AX10479, the phenyl amide of 4-hydroxy-8-methanesulfonylamino-quinoline-2- carboxylic acid, was identified as a Zn2+-dependent, 27 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.
