| Literature DB >> 29439904 |
Yong-Jin Wu1, Jason Guernon2, Andrea McClure2, Brian Venables2, Ramkumar Rajamani2, Kevin J Robbins2, Ronald J Knox2, Michele Matchett2, Rick L Pieschl2, James Herrington2, Linda J Bristow2, Nicholas A Meanwell2, Richard Olson2, Lorin A Thompson2, Carolyn Dzierba2.
Abstract
Replacement of the piperidine ring in the lead benzenesulfonamide Nav1.7 inhibitor 1 with a weakly basic morpholine core resulted in a significant reduction in Nav1.7 inhibitory activity, but the activity was restored by shortening the linkage from methyleneoxy to oxygen. These efforts led to a series of morpholine-based aryl sulfonamides as isoform-selective Nav1.7 inhibitors. This report describes the synthesis and SAR of these analogs.Entities:
Keywords: Aryl sulfonamides; Morpholine-based; Na(v)1.7 inhibitor; Pain
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Year: 2018 PMID： 29439904 DOI： 10.1016/j.bmcl.2018.01.035
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823