title: Aryl sulfonamido indane inhibitors of the Kv1.5 ion channel.
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.
authors.affiliation: Icagen Inc., PO Box 14487, Research Triangle Park, NC 27709, USA.
authors.forename: Michael F
authors.initials: MF
authors.lastname: Gross
authors.forename: Serge
authors.initials: S
authors.lastname: Beaudoin
authors.forename: Grant
authors.initials: G
authors.lastname: McNaughton-Smith
authors.forename: George S
authors.initials: GS
authors.lastname: Amato
authors.forename: Neil A
authors.initials: NA
authors.lastname: Castle
authors.forename: Christine
authors.initials: C
authors.lastname: Huang
authors.forename: Anruo
authors.initials: A
authors.lastname: Zou
authors.forename: Weifeng
authors.initials: W
authors.lastname: Yu
mesh_terms: 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*
chemical_list: D007189:Indans; D051666:Kv1.5 Potassium Channel; D026902:Potassium Channel Blockers; D013449:Sulfonamides; C093582:indan