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Updated: May 17, 2026

Real-time Imaging of Leukotriene B4 Mediated Cell Migration and BLT1 Interactions with β-arrestin
Published on: December 23, 2010
Azabenzthiazole inhibitors of leukotriene A₄ hydrolase
Virginia M Tanis1, Genesis M Bacani, Jonathan M Blevitt
1Janssen Research & Development LLC, 3210 Merryfield Row, San Diego, CA 92121, United States. vtanis@its.jnj.com
Abstract:
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.
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