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Bioorg Med Chem Lett. 2013 Mar 1;23(5):1553-6. doi: 10.1016/j.bmcl.2012.11.048. Epub 2012 Dec 8.

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

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  • 1ActivX Biosciences, Inc., 11025 N. Torrey Pines Road, La Jolla, CA 92037, USA.

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.

Copyright © 2012 Elsevier Ltd. All rights reserved.

PMID:
23333209
[PubMed - indexed for MEDLINE]
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