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Discovery of isoxazole voltage gated sodium channel blockers for treatment of chronic pain

Authors :
Ying-Duo Gao
Maria L. Garcia
Xiaohua Li
Catherine Abbadie
Daniel R. McMasters
Feng Ye
Brande S. Williams
William J. Martin
Kathryn A. Lyons
Ann E. Weber
Gregory J. Kaczorowski
John P. Felix
McHardy M. Smith
Shao Pengcheng Patrick
William H. Parsons
Birgit T. Priest
Erin McGowan
Source :
Bioorganic & Medicinal Chemistry Letters. 19:5334-5338
Publication Year :
2009
Publisher :
Elsevier BV, 2009.

Abstract

A series of novel isoxazole voltage gated sodium channel blockers have been synthesized and evaluated. Substitutions on the benzylic position of benzamide were investigated to determine their effect on Na(v)1.7 inhibitory potency. The spirocyclobutyl substitution had the most significant enhancement on Na(v)1.7 inhibitory activity.

Details

ISSN :
0960894X
Volume :
19
Database :
OpenAIRE
Journal :
Bioorganic & Medicinal Chemistry Letters
Accession number :
edsair.doi.dedup.....701dc8af84f883465fcabf2285c21877
Full Text :
https://doi.org/10.1016/j.bmcl.2009.07.135