Sulfonamides as Selective Na(V)1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement

[Image: see text] Human genetic evidence has identified the voltage-gated sodium channel Na(V)1.7 as an attractive target for the treatment of pain. We initially identified naphthalene sulfonamide 3 as a potent and selective inhibitor of Na(V)1.7. Optimization to reduce biliary clearance by balancin...

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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: Marx, Isaac E., Dineen, Thomas A., Able, Jessica, Bode, Christiane, Bregman, Howard, Chu-Moyer, Margaret, DiMauro, Erin F., Du, Bingfan, Foti, Robert S., Fremeau, Robert T., Gao, Hua, Gunaydin, Hakan, Hall, Brian E., Huang, Liyue, Kornecook, Thomas, Kreiman, Charles R., La, Daniel S., Ligutti, Joseph, Lin, Min-Hwa Jasmine, Liu, Dong, McDermott, Jeff S., Moyer, Bryan D., Peterson, Emily A., Roberts, Jonathan T., Rose, Paul, Wang, Jean, Youngblood, Beth D., Yu, Violeta, Weiss, Matthew M.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2016
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC5150675/
https://ncbi.nlm.nih.gov/pubmed/27994738
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.6b00243
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