PubMed 16949818

Referenced in Channelpedia wiki pages of: none

Automatically associated channels: Kv1.5

Title: Potent antagonists of the Kv1.5 potassium channel: synthesis and evaluation of analogous N,N-diisopropyl-2-(pyridine-3-yl)acetamides.

Authors: Kausik K Nanda, M Brad Nolt, Matthew J Cato, Stefanie A Kane, Laszlo Kiss, Robert H Spencer, Jixin Wang, Joseph J Lynch, Christopher P Regan, Gary L Stump, Bing Li, Rebecca White, Suzie Yeh, Michael J Bogusky, Mark T Bilodeau, Christopher J Dinsmore, Craig W Lindsley, George D Hartman, Scott E Wolkenberg, B Wesley Trotter

Journal, date & volume: Bioorg. Med. Chem. Lett., 2006 Nov 15 , 16, 5897-901

PubMed link:

This letter describes the discovery of a novel series of potent Kv1.5 ion channel antagonists based on a diisopropyl amide scaffold. Structure-activity relationships of functionalized analogs are discussed. Key compound 1-(3-(diisopropylcarbamoyl)-2-phenyl-3-(pyridin-3-yl)propyl)-3-(2-fluorobenzyl)urea (10) exhibits significant atrial-selective effects in an in vivo model.