| Literature DB >> 30576602 |
Guanglin Luo1, Ling Chen1, Amy Easton1, Amy Newton1, Clotilde Bourin1, Eric Shields1, Kathy Mosure1, Matthew G Soars1, Ronald J Knox1, Michele Matchett1, Rick L Pieschl1, Debra J Post-Munson1, Shuya Wang1, James Herrington1, John Graef1, Kimberly Newberry1, Digavalli V Sivarao1, Arun Senapati1, Linda J Bristow1, Nicholas A Meanwell1, Lorin A Thompson1, Carolyn Dzierba1.
Abstract
3-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.Entities:
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Year: 2019 PMID： 30576602 DOI： 10.1021/acs.jmedchem.8b01550
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446