jm8b01550_si_001.csv (4.44 kB)
Discovery of Indole- and Indazole-acylsulfonamides as Potent and Selective NaV1.7 Inhibitors for the Treatment of Pain
dataset
posted on 2018-12-21, 00:00 authored by Guanglin Luo, Ling Chen, Amy Easton, Amy Newton, Clotilde Bourin, Eric Shields, Kathy Mosure, Matthew G. Soars, Ronald J. Knox, Michele Matchett, Rick L. Pieschl, Debra J. Post-Munson, Shuya Wang, James Herrington, John Graef, Kimberly Newberry, Digavalli V. Sivarao, Arun Senapati, Linda J. Bristow, Nicholas A. Meanwell, Lorin A. Thompson, Carolyn Dzierba3-Aryl-indole and 3-aryl-indazole
derivatives were identified as
potent and selective Nav1.7 inhibitors. Compound 29 was shown to be efficacious in the mouse formalin assay
and also reduced complete Freund’s adjuvant (CFA)-induced thermal
hyperalgesia and chronic constriction injury (CCI) induced cold allodynia
and models of inflammatory and neuropathic pain, respectively, following
intraperitoneal (IP) doses of 30 mg/kg. The observed efficacy could
be correlated with the mouse dorsal root ganglion exposure and NaV1.7 potency associated with 29.
