Aryl sulfonamido indane inhibitors of the Kv1.5 ion channel

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 IC50 of 0.033 μM against Kv1.5 and is selective against other cardiac ion channels, including hERG.

Structure–activity relationship of a new class of Kv1.5 inhibitors based on the indane scaffold was investigated.Figure optionsDownload as PowerPoint slide