Channelpedia

PubMed 15125940


Referenced in Channelpedia wiki pages of: none

Automatically associated channels: Kv1.5 , Kv11.1



Title: Pharmacophore-based search, synthesis, and biological evaluation of anthranilic amides as novel blockers of the Kv1.5 channel.

Authors: Stefan Peukert, Joachim Brendel, Bernard Pirard, Carsten Strübing, Heinz-Werner Kleemann, Thomas Böhme, Horst Hemmerle

Journal, date & volume: Bioorg. Med. Chem. Lett., 2004 Jun 7 , 14, 2823-7

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/15125940


Abstract
The search for novel, potent Kv1.5 blockers based on an anthranilic amide scaffold employing a pharmacophore-based virtual screening approach is described. The synthesis and structure-activity relationships (SAR) with respect to inhibition of the Kv1.5 channel are discussed. The most potent compounds display sub-micromolar inhibition of Kv1.5 and no significant effect on the HERG channel. In addition, good oral bioavailability is demonstrated for compound 3i in rats.