Referenced in: none

Automatically associated channels: Kv1.5

Title: Lactam sulfonamides as potent inhibitors of the Kv1.5 potassium ion channel.

Authors: Roine I Olsson, Ingemar Jacobson, Tommy Iliefski, Jonas Boström, Öjvind Davidsson, Ola Fjellström, Annika Björe, Christina Olsson, Johan Sundell, Ulrik Gran, Jonna Gyll, Jesper Malmberg, Olle Hidestål, Hans Emtenäs, Tor Svensson, Zhong-Qing Yuan, Gert Strandlund, Annika Astrand, Emma Lindhardt, Gunilla Linhardt, Elin Forsström, Ågot Högberg, Frida Persson, Birgit Andersson, Anna Rönnborg, Boel Löfberg

Journal, date & volume: Bioorg. Med. Chem. Lett., 2014 Mar 1 , 24, 1269-73

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/24513046

Abstract
A series of lactam sulfonamides has been discovered and optimized as inhibitors of the Kv1.5 potassium ion channel for treatment of atrial fibrillation. In vitro structure-activity relationships from lead structure C to optimized structure 3y are described. Compound 3y was evaluated in a rabbit PD-model and was found to selectively prolong the atrial effective refractory period at submicromolar concentrations.