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 Molloy, Margery A. Chaikin, Carl L. Manthey, Mark R. Player, Bruce E. Tomczuk, Sanath K. Meegalla

Research output: Contribution to journalArticle

10 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)3925-3929
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number13
DOIs
StatePublished - May 31 2010
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Fingerprint Dive into the research topics of 'Reducing ion channel activity in a series of 4-heterocyclic arylamide FMS inhibitors'. Together they form a unique fingerprint.

  • Cite this

    Wilson, K. J., Illig, C. R., Chen, J., Wall, M. J., Ballentine, S. K., Desjarlais, R. L., Chen, Y., Schubert, C., Donatelli, R., Petrounia, I., Crysler, C. S., Molloy, C., Chaikin, M. A., Manthey, C. L., Player, M. R., Tomczuk, B. E., & Meegalla, S. K. (2010). Reducing ion channel activity in a series of 4-heterocyclic arylamide FMS inhibitors. Bioorganic and Medicinal Chemistry Letters, 20(13), 3925-3929. https://doi.org/10.1016/j.bmcl.2010.05.013