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Issue 6, 2017
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The discovery of a potent Nav1.3 inhibitor with good oral pharmacokinetics

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Abstract

In this article, we describe the discovery of an aryl ether series of potent and selective Nav1.3 inhibitors. Based on structural analogy to a similar series of compounds we have previously shown bind to the domain IV voltage sensor region of Nav channels, we propose this series binds in the same location. We describe the development of this series from a published starting point, highlighting key selectivity and potency data, and several studies designed to validate Nav1.3 as a target for pain.

Graphical abstract: The discovery of a potent Nav1.3 inhibitor with good oral pharmacokinetics

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Article information


Submitted
14 Mar 2017
Accepted
26 Apr 2017
First published
28 Apr 2017

Med. Chem. Commun., 2017,8, 1255-1267
Article type
Research Article

The discovery of a potent Nav1.3 inhibitor with good oral pharmacokinetics

D. C. Pryde, N. A. Swain, P. A. Stupple, C. W. West, B. Marron, C. J. Markworth, D. Printzenhoff, Z. Lin, P. J. Cox, R. Suzuki, S. McMurray, G. J. Waldron, C. E. Payne, J. S. Warmus and M. L. Chapman, Med. Chem. Commun., 2017, 8, 1255
DOI: 10.1039/C7MD00131B

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