Reducing ion channel activity in a series of 4-heterocyclic arylamide FMS inhibitors.
Kenneth J Wilson, 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
Johnson & Johnson Pharmaceutical Research & Development, Spring House, PA 19477, USA. kwilso10@its.jnj.com
Bioorganic & medicinal chemistry letters 2010 Jul 1During 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. 2010 Elsevier Ltd. All rights reserved.
Citation
Kenneth J Wilson, 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. Reducing ion channel activity in a series of 4-heterocyclic arylamide FMS inhibitors. Bioorganic & medicinal chemistry letters. 2010 Jul 1;20(13):3925-9
Mesh Tags
Substances
PMID: 20570147
View Full Text
