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 IC(50) of 0.033microM against Kv1.5 and is selective against other cardiac ion channels, including hERG.
Gross
Michael F
MF
Icagen Inc., PO Box 14487, Research Triangle Park, NC 27709, USA.
Beaudoin
Serge
S
McNaughton-Smith
Grant
G
Amato
George S
GS
Castle
Neil A
NA
Huang
Christine
C
Zou
Anruo
A
Yu
Weifeng
W
D000818:Animals; D007189:Indans / Q000138:chemical synthesis / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D051666:Kv1.5 Potassium Channel / Q000037:antagonists & inhibitors* / Q000378:metabolism; D051379:Mice; D015394:Molecular Structure; D026902:Potassium Channel Blockers / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D007189:Indans; D051666:Kv1.5 Potassium Channel; D026902:Potassium Channel Blockers; D013449:Sulfonamides; C093582:indan