Discovery of a novel class of biphenyl pyrazole sodium channel blockers for treatment of neuropathic pain.

Sriram Tyagarajan,Prasun K. Chakravarty,Bishan Zhou,Brett Taylor,Ronsar Eid,Michael H. Fisher,William H. Parsons,Mathew J. Wyvratt,Kathryn A. Lyons,Tracy Klatt,Xiaohua Li,Sanjeev Kumar,Brande S. Williams,John P. Felix,Birgit T. Priest,Richard M. Brochu,Vivien A. Warren,McHardy M. Smith,Maria L. Garcia,Gregory J. Kaczorowski,William J. Martin,Catherine Abbadie,Erin McGowan,Nina Jochnowitz,Ann E. Weber,Joseph L. Duffy

Discovery of a novel class of biphenyl pyrazole sodium channel blockers for treatment of neuropathic pain.

2010

A series of novel biphenyl pyrazole dicarboxamides were identified as potential sodium channel blockers for treatment of neuropathic pain. Compound 20 had outstanding efficacy in the Chung rat spinal nerve ligation (SNL) model of neuropathic pain.

Keywords:

Pyrazole
Sodium channel blocker
In vivo
Stereochemistry
Biochemistry
Ligation
Pharmacology
Chemistry
Spinal nerve
Pharmacokinetics
Analgesic
Neuropathic pain
biphenyl derivatives
metabolic stability
spinal nerve ligation

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