Format

Send to

Choose Destination
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.

Author information

1
Janssen 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.

PMID:
23127888
DOI:
10.1016/j.bmcl.2012.10.036
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center