Amides of 4-hydroxy-8-methanesulfonylamino-quinoline-2-carboxylic acid as zinc-dependent inhibitors of Lp-PLA₂

Autor:	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
Rok vydání:	2012
Předmět:	Structure-Activity Relationship Zinc 1-Alkyl-2-acetylglycerophosphocholine Esterase Quinolines Humans Stereoisomerism Amides
Zdroj:	Bioorganicmedicinal chemistry letters. 23(5)
ISSN:	1464-3405
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=pmid________::b34b44aa3a62c9cf8f531166843fd435 https://pubmed.ncbi.nlm.nih.gov/23333209 Zobrazit plný text záznamu Full Text from ScienceDirect