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

Authors :
Shelley K. Ballentine
Ioanna Petrounia
Yanmin Chen
Carsten Schubert
Sanath K. Meegalla
Bruce E. Tomczuk
Robert R. Donatelli
Christopher J. Molloy
Jinsheng Chen
Margery A. Chaikin
Carl R. Illig
Mark R. Player
Renee L. DesJarlais
Mark J. Wall
Carl Crysler
Kenneth J. Wilson
Carl L. Manthey
Source :
Bioorganicmedicinal chemistry letters. 20(13)
Publication Year :
2010

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.

Details

ISSN :
14643405
Volume :
20
Issue :
13
Database :
OpenAIRE
Journal :
Bioorganicmedicinal chemistry letters
Accession number :
edsair.doi.dedup.....8c5510c9a3e081ba95d9c48c2a863b4c