2. Academic Validation
  3. Discovery of triarylethanolamine inhibitors of the Kv1.5 potassium channel

Discovery of triarylethanolamine inhibitors of the Kv1.5 potassium channel

  • Bioorg Med Chem Lett. 2010 Apr 15;20(8):2493-6. doi: 10.1016/j.bmcl.2010.03.005.
Douglas C Beshore 1,  Nigel J Liverton,  Charles J McIntyre,  Christopher F Claiborne,  Brian Libby,  J Christopher Culberson,  Joseph J Salata,  Christopher P Regan,  Joseph J Lynch,  Laszlo Kiss,  Robert H Spencer,  Stephanie A Kane,  Rebecca B White,  Suzie Yeh,  George D Hartman,  Christopher J Dinsmore
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., Inc., West Point, PA 19486, USA. douglas_beshore@merck.com
PMID: 20304642 DOI: 10.1016/j.bmcl.2010.03.005
Abstract

A series of triarylethanolamine inhibitors of the Kv1.5 Potassium Channel have been prepared and evaluated for their effects in vitro and in vivo. The structure-activity relationship (SAR) studies described herein led to the development of potent, selective and orally active inhibitors of Kv1.5.

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