Aryl sulfonamido indane inhibitors of the Kv1.5 ion channel

Michael F Gross; Serge Beaudoin; Grant McNaughton-Smith; George S Amato; Neil A Castle; Christine Huang; Anruo Zou; Weifeng Yu

doi:10.1016/j.bmcl.2007.02.052

Aryl sulfonamido indane inhibitors of the Kv1.5 ion channel

Bioorg Med Chem Lett. 2007 May 15;17(10):2849-53. doi: 10.1016/j.bmcl.2007.02.052. Epub 2007 Feb 27.

Authors

Michael F Gross¹, Serge Beaudoin, Grant McNaughton-Smith, George S Amato, Neil A Castle, Christine Huang, Anruo Zou, Weifeng Yu

Affiliation

¹ Icagen Inc., PO Box 14487, Research Triangle Park, NC 27709, USA.

PMID: 17350840
DOI: 10.1016/j.bmcl.2007.02.052

Abstract

A collection of aryl sulfonamido indanes based on the lead compound 1 was synthesized and evaluated for Kv1.5 inhibitory activity. Kv1.5 inhibitors have the potential to be atrium-selective agents for treatment of atrial fibrillation. (1R,2R)-1 has an IC(50) of 0.033microM against Kv1.5 and is selective against other cardiac ion channels, including hERG.

Publication types

Evaluation Study

MeSH terms

Animals
Indans / chemical synthesis
Indans / pharmacology
Inhibitory Concentration 50
Kv1.5 Potassium Channel / antagonists & inhibitors*
Kv1.5 Potassium Channel / metabolism
Mice
Molecular Structure
Potassium Channel Blockers / chemical synthesis*
Potassium Channel Blockers / pharmacology*
Structure-Activity Relationship
Sulfonamides / chemical synthesis*
Sulfonamides / chemistry
Sulfonamides / pharmacology*

Substances

Indans
Kv1.5 Potassium Channel
Potassium Channel Blockers
Sulfonamides
indan