Literature DB >> 20570147

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

Kenneth J Wilson1, 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.   

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. 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20570147     DOI: 10.1016/j.bmcl.2010.05.013

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Synthesis and Selective Functionalization of Thiadiazine 1,1-Dioxides with Efficacy in a Model of Huntington's Disease.

Authors:  Leila Terrab; Christopher J Rosenker; Lisa Johnstone; Linh K Ngo; Li Zhang; Nathaniel F Ware; Bettina Miller; Andrea Z Topacio; Sara Sannino; Jeffrey L Brodsky; Peter Wipf
Journal:  ACS Med Chem Lett       Date:  2020-02-20       Impact factor: 4.345

2.  Development of a rapid streptavidin capture-based assay for the tyrosine phosphorylated CSF-1R in peripheral blood mononuclear cells.

Authors:  Shalini Chaturvedi; Elayne Dell; Derick Siegel; Gregory Brittingham; Shobha Seetharam
Journal:  Int J Biol Sci       Date:  2013-11-22       Impact factor: 6.580

  2 in total

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