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  • Title: Reducing ion channel activity in a series of 4-heterocyclic arylamide FMS inhibitors.
    Author: Wilson KJ, Illig CR, Chen J, Wall MJ, Ballentine SK, DesJarlais RL, Chen Y, Schubert C, Donatelli R, Petrounia I, Crysler CS, Molloy CJ, Chaikin MA, Manthey CL, Player MR, Tomczuk BE, Meegalla SK.
    Journal: Bioorg Med Chem Lett; 2010 Jul 01; 20(13):3925-9. PubMed ID: 20570147.
    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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