Referenced in: none

Automatically associated channels: Kv1.5

Title: Synthesis and evaluation of diphenylphosphinic amides and diphenylphosphine oxides as inhibitors of Kv1.5.

Authors: Roine I Olsson, Ingemar Jacobson, Jonas Boström, Tomas Fex, Annika Björe, Christina Olsson, Johan Sundell, Ulrik Gran, Anna Ohrn, Andreas Nordin, Jonna Gyll, Maria Thorstensson, Ahlke Hayen, Karolina Aplander, Olle Hidestål, Fanyi Jiang, Gunilla Linhardt, Elin Forsström, Teresa Collins, Monika Sundqvist, Emma Lindhardt, Annika Strand, Boel Löfberg

Journal, date & volume: Bioorg. Med. Chem. Lett., 2013 Feb 1 , 23, 706-10

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/23260347

Abstract
Diphenylphosphinic amides and diphenylphosphine oxides have been synthesized and tested as inhibitors of the Kv1.5 potassium ion channel as a possible treatment for atrial fibrillation. In vitro structure-activity relationships are discussed and several compounds with Kv1.5 IC(50) values of <0.5 μM were discovered. Selectivity over the ventricular IKs current was monitored and selective compounds were found. Results from a rabbit PD-model are included.