10.1021/acs.jmedchem.8b01550.s001
Guanglin Luo
Guanglin
Luo
Ling Chen
Ling
Chen
Amy Easton
Amy
Easton
Amy Newton
Amy
Newton
Clotilde Bourin
Clotilde
Bourin
Eric Shields
Eric
Shields
Kathy Mosure
Kathy
Mosure
Matthew G. Soars
Matthew G.
Soars
Ronald J. Knox
Ronald J.
Knox
Michele Matchett
Michele
Matchett
Rick L. Pieschl
Rick L.
Pieschl
Debra J. Post-Munson
Debra J.
Post-Munson
Shuya Wang
Shuya
Wang
James Herrington
James
Herrington
John Graef
John
Graef
Kimberly Newberry
Kimberly
Newberry
Digavalli V. Sivarao
Digavalli V.
Sivarao
Arun Senapati
Arun
Senapati
Linda J. Bristow
Linda
J. Bristow
Nicholas A. Meanwell
Nicholas A.
Meanwell
Lorin A. Thompson
Lorin A.
Thompson
Carolyn Dzierba
Carolyn
Dzierba
Discovery of Indole-
and Indazole-acylsulfonamides
as Potent and Selective Na<sub>V</sub>1.7 Inhibitors for the Treatment
of Pain
American Chemical Society
2018
Pain 3- Aryl-indole
CCI
mouse formalin assay
Na v 1.7 inhibitors
IP
Na V 1.7 potency
Compound 29
Selective Na V 1.7 Inhibitors
constriction injury
CFA
mouse dorsal root ganglion exposure
3- aryl-indazole derivatives
neuropathic pain
2018-12-21 00:00:00
Dataset
https://acs.figshare.com/articles/dataset/Discovery_of_Indole-_and_Indazole-acylsulfonamides_as_Potent_and_Selective_Na_sub_V_sub_1_7_Inhibitors_for_the_Treatment_of_Pain/7562126
3-Aryl-indole and 3-aryl-indazole
derivatives were identified as
potent and selective Na<sub>v</sub>1.7 inhibitors. Compound <b>29</b> 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 Na<sub>V</sub>1.7 potency associated with <b>29</b>.