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Bioorg Med Chem Lett. 2012 Dec 15;22(24):7504-11. doi: 10.1016/j.bmcl.2012.10.036. Epub 2012 Oct 17.

Azabenzthiazole inhibitors of leukotriene A₄ hydrolase.

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  • 1Janssen Research & Development LLC, 3210 Merryfield Row, San Diego, CA 92121, United States.


Previously, benzthiazole containing LTA(4)H inhibitors were discovered that were potent (1-3), but were associated with the potential for a hERG liability. Utilizing medicinal chemistry first principles (e.g., introducing rigidity, lowering cLogD) a new benzthiazole series was designed, congeners of 1-3, which led to compounds 7a, 7c, 12a-d which exhibited LTA(4)H IC(50)=3-6 nM and hERG Dofetilide Binding IC(50)=8.9-> >10 μM.

Copyright © 2012 Elsevier Ltd. All rights reserved.

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