title: Discovery and synthesis of tetrahydroindolone-derived carbamates as Kv1.5 blockers.
abstract: A novel class of tetrahydroindolone-derived carbamates has been discovered whose members are potent Kv1.5 blockers. The in vitro data show that compounds 6 and 29 are quite potent. They are also very selective over hERG (>450-fold) and L-type calcium channels (>450-fold).
authors.affiliation: Procter and Gamble Pharmaceuticals, Mason Business Center, 8700 Mason-Montgomery Road, Mason, OH 45040, USA. fluxe_cj@yahoo.com
authors.forename: Andrew
authors.initials: A
authors.lastname: Fluxe
authors.forename: Shengde
authors.initials: S
authors.lastname: Wu
authors.forename: James B
authors.initials: JB
authors.lastname: Sheffer
authors.forename: John M
authors.initials: JM
authors.lastname: Janusz
authors.forename: Michael
authors.initials: M
authors.lastname: Murawsky
authors.forename: Gina M
authors.initials: GM
authors.lastname: Fadayel
authors.forename: Bin
authors.initials: B
authors.lastname: Fang
authors.forename: Michelle
authors.initials: M
authors.lastname: Hare
authors.forename: Laurent
authors.initials: L
authors.lastname: Djandjighian
mesh_terms: D020746:Calcium Channels, L-Type / Q000494:pharmacology; D002219:Carbamates / Q000737:chemistry* / Q000494:pharmacology*; D000072237:ERG1 Potassium Channel; D051638:Ether-A-Go-Go Potassium Channels / Q000494:pharmacology; D006801:Humans; D007211:Indoles / Q000737:chemistry* / Q000494:pharmacology*; D051666:Kv1.5 Potassium Channel / Q000037:antagonists & inhibitors*; D026902:Potassium Channel Blockers / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D020746:Calcium Channels, L-Type; D002219:Carbamates; D000072237:ERG1 Potassium Channel; D051638:Ether-A-Go-Go Potassium Channels; D007211:Indoles; C000606913:KCNH2 protein, human; D051666:Kv1.5 Potassium Channel; D026902:Potassium Channel Blockers