Discovery and hit-to-lead evaluation of piperazine amides as selective, state-dependent NaV1.7 inhibitorsThe authors declare no competing financial interests.Electronic supplementary information (ESI) available: Assay protocols, experimental procedures, spectra of key compounds. See DOI: 10.1039/c6md00578k

Na V 1.7 is a particularly compelling target for the treatment of pain. Herein, we report the discovery and evaluation of a series of piperazine amides that exhibit state-dependent inhibition of Na V 1.7. After demonstrating significant pharmacodynamic activity with early lead compound 14 in a Na V...

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Hauptverfasser:	Sparling, Brian A, Yi, S, Able, J, Bregman, H, DiMauro, Erin F, Foti, R. S, Gao, H, Guzman-Perez, A, Huang, H, Jarosh, M, Kornecook, T, Ligutti, J, Milgram, B. C, Moyer, B. D, Youngblood, B, Yu, V. L, Weiss, M. M
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Sprache:	eng
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