Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1373797 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
Voltage-gated sodium channels have been shown to play a critical role in neuropathic pain. A series of low molecular weight biaryl substituted pyrazole carboxamides were identified with good in-vitro potency and in-vivo efficacy. Compound 26, a Nav1.7 blocker has excellent efficacy in the Chung model of neuropathic pain.
Graphical abstractA series of low molecular weight biaryl substituted pyrazoles with good in-vitro potency and in-vivo efficacy were identified as Nav1.7 blockers. These state dependent sodium channel blockers were synthesized and evaluated for treatment of neuropathic pain.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Sriram Tyagarajan, Prasun K. Chakravarty, Bishan Zhou, Brett Taylor, Michael H. Fisher, Mathew J. Wyvratt, Kathy Lyons, Tracy Klatt, Xiaohua Li, Sanjeev Kumar, Brande Williams, John Felix, Birgit T. Priest, Richard M. Brochu, Vivien Warren,