Discovery of non-zwitterionic aryl sulfonamides as Nav1.7 inhibitors with efficacy in preclinical behavioral models and translational measures of nociceptive neuron activation

Yong Jin Wu; Jason Guernon; Andrea McClure; Guanglin Luo; Ramkumar Rajamani; Alicia Ng; Amy Easton; Amy Newton; Clotilde Bourin; Dawn Parker; Kathleen Mosure; Omar Barnaby; Matthew G. Soars; Ronald J. Knox; Michele Matchett; Rick Pieschl; James Herrington; Ping Chen; D. V. Sivarao; Linda J. Bristow; Nicholas A. Meanwell; Joanne Bronson; Richard Olson; Lorin A. Thompson; Carolyn Dzierba

doi:10.1016/j.bmc.2017.08.012

Discovery of non-zwitterionic aryl sulfonamides as Na_v1.7 inhibitors with efficacy in preclinical behavioral models and translational measures of nociceptive neuron activation

Yong Jin Wu
, Jason Guernon
, Andrea McClure
, Guanglin Luo
, Ramkumar Rajamani
, Alicia Ng
, Amy Easton
, Amy Newton
, Clotilde Bourin
, Dawn Parker
, Kathleen Mosure
, Omar Barnaby
, Matthew G. Soars
, Ronald J. Knox
, Michele Matchett
, Rick Pieschl
, James Herrington
, Ping Chen
, D. V. Sivarao
, Linda J. Bristow

Nicholas A. Meanwell, Joanne Bronson, Richard Olson, Lorin A. Thompson, Carolyn Dzierba

Department of Pharmaceutical Sciences

Bristol-Myers Squibb

Research output: Contribution to journal › Article › peer-review

Original language	English
Pages (from-to)	5490-5505
Number of pages	16
Journal	Bioorganic and Medicinal Chemistry
Volume	25
Issue number	20
DOIs	https://doi.org/10.1016/j.bmc.2017.08.012
State	Published - 2017

ASJC Scopus Subject Areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

Keywords

Benzenesulfonamide
Membrane permeability
Na1.7 inhibitor
Neuropathic and inflammatory pain
Nociceptive flexion reflex (NFR)
Translational electromyogram

Access to Document

10.1016/j.bmc.2017.08.012

Cite this

Wu, Y. J., Guernon, J., McClure, A., Luo, G., Rajamani, R., Ng, A., Easton, A., Newton, A., Bourin, C., Parker, D., Mosure, K., Barnaby, O., Soars, M. G., Knox, R. J., Matchett, M., Pieschl, R., Herrington, J., Chen, P., Sivarao, D. V., ... Dzierba, C. (2017). Discovery of non-zwitterionic aryl sulfonamides as Na_v1.7 inhibitors with efficacy in preclinical behavioral models and translational measures of nociceptive neuron activation. Bioorganic and Medicinal Chemistry, 25(20), 5490-5505. https://doi.org/10.1016/j.bmc.2017.08.012

Discovery of non-zwitterionic aryl sulfonamides as Na_v1.7 inhibitors with efficacy in preclinical behavioral models and translational measures of nociceptive neuron activation. / Wu, Yong Jin; Guernon, Jason; McClure, Andrea et al.
In: Bioorganic and Medicinal Chemistry, Vol. 25, No. 20, 2017, p. 5490-5505.

Research output: Contribution to journal › Article › peer-review

Wu, YJ, Guernon, J, McClure, A, Luo, G, Rajamani, R, Ng, A, Easton, A, Newton, A, Bourin, C, Parker, D, Mosure, K, Barnaby, O, Soars, MG, Knox, RJ, Matchett, M, Pieschl, R, Herrington, J, Chen, P, Sivarao, DV, Bristow, LJ, Meanwell, NA, Bronson, J, Olson, R, Thompson, LA & Dzierba, C 2017, 'Discovery of non-zwitterionic aryl sulfonamides as Na_v1.7 inhibitors with efficacy in preclinical behavioral models and translational measures of nociceptive neuron activation', Bioorganic and Medicinal Chemistry, vol. 25, no. 20, pp. 5490-5505. https://doi.org/10.1016/j.bmc.2017.08.012

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AU - Luo, Guanglin

AU - Rajamani, Ramkumar

AU - Ng, Alicia

AU - Easton, Amy

AU - Newton, Amy

AU - Bourin, Clotilde

AU - Parker, Dawn

AU - Mosure, Kathleen

AU - Barnaby, Omar

AU - Soars, Matthew G.

AU - Knox, Ronald J.

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AU - Chen, Ping

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AU - Bristow, Linda J.

AU - Meanwell, Nicholas A.

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AU - Olson, Richard

AU - Thompson, Lorin A.

AU - Dzierba, Carolyn

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KW - Na1.7 inhibitor

KW - Neuropathic and inflammatory pain

KW - Nociceptive flexion reflex (NFR)

KW - Translational electromyogram

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