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Bioorg Med Chem Lett. 2012 Jan 15;22(2):868-71. doi: 10.1016/j.bmcl.2011.12.045. Epub 2011 Dec 13.

Amides of xanthurenic acid as zinc-dependent inhibitors of Lp-PLA(2).

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


AX10185, the phenyl amide of xanthurenic acid, was found to be a sub-100nM inhibitor of Lp-PLA(2). However, in the presence of EDTA the inhibitory activity of AX10185 was extinguished while the enzymatic activity of Lp-PLA(2) did not change. Subsequent metal screening experiments determined the inhibition to be Zn(2+) dependent. Structure-activity relationship studies indicated the presence of the 4-hydroxy group to be critical and selected substituted phenyl, polycyclic, and cycloaliphatic amides of xanthurenic acid to be well tolerated.

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