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
  • 1. Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., Inc., West Point, PA 19486, USA. [email protected]
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.