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Merck

Aryl sulfonamido indane inhibitors of the Kv1.5 ion channel.

Bioorganic & medicinal chemistry letters (2007-03-14)
Michael F Gross, Serge Beaudoin, Grant McNaughton-Smith, George S Amato, Neil A Castle, Christine Huang, Anruo Zou, Weifeng Yu
PMID17350840
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.