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. 2010 Jul 1;20(13):3925-9.
doi: 10.1016/j.bmcl.2010.05.013. Epub 2010 May 12.

Reducing ion channel activity in a series of 4-heterocyclic arylamide FMS inhibitors

Kenneth J Wilson  1 , Carl R Illig, Jinsheng Chen, Mark J Wall, Shelley K Ballentine, Renee L DesJarlais, Yanmin Chen, Carsten Schubert, Robert Donatelli, Ioanna Petrounia, Carl S Crysler, Christopher J Molloy, Margery A Chaikin, Carl L Manthey, Mark R Player, Bruce E Tomczuk, Sanath K Meegalla
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Reducing ion channel activity in a series of 4-heterocyclic arylamide FMS inhibitors

Kenneth J Wilson et al. Bioorg Med Chem Lett. .

Abstract

During efforts to improve the bioavailability of FMS kinase inhibitors 1 and 2, a series of saturated and aromatic 4-heterocycles of reduced basicity were prepared and evaluated in an attempt to also improve the cardiovascular safety profile over lead arylamide 1, which possessed ion channel activity. The resultant compounds retained excellent potency and exhibited diminished ion channel activity.

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