title: Discovery and in vitro/in vivo studies of tetrazole derivatives as Kv1.5 blockers.
abstract: A novel class of tetrazole-derived Kv1.5 blockers is disclosed. In in vitro studies, several compounds had IC(50)s ranging from 180 to 550 nM. In vivo studies indicated that compounds 2f and 2j increased right atrial ERP about 40% without affecting ventricular ERP.
authors.affiliation: Procter & Gamble Pharmaceuticals, Health Care Research Center, 8700 Mason-Montgomery Road, Mason, OH 45040, USA. wu.s.3@pg.com
authors.forename: Shengde
authors.initials: S
authors.lastname: Wu
authors.forename: Andrew
authors.initials: A
authors.lastname: Fluxe
authors.forename: Jim
authors.initials: J
authors.lastname: Sheffer
authors.forename: John M
authors.initials: JM
authors.lastname: Janusz
authors.forename: Benjamin E
authors.initials: BE
authors.lastname: Blass
authors.forename: Ron
authors.initials: R
authors.lastname: White
authors.forename: Chris
authors.initials: C
authors.lastname: Jackson
authors.forename: Richard
authors.initials: R
authors.lastname: Hedges
authors.forename: Michael
authors.initials: M
authors.lastname: Murawsky
authors.forename: Bin
authors.initials: B
authors.lastname: Fang
authors.forename: Gina M
authors.initials: GM
authors.lastname: Fadayel
authors.forename: Michelle
authors.initials: M
authors.lastname: Hare
authors.forename: Laurent
authors.initials: L
authors.lastname: Djandjighian
mesh_terms: D000818:Animals; D006339:Heart Rate / Q000187:drug effects; D007700:Kinetics; D051666:Kv1.5 Potassium Channel / Q000037:antagonists & inhibitors*; D008958:Models, Molecular; D013329:Structure-Activity Relationship; D013552:Swine; D013556:Swine, Miniature; D013777:Tetrazoles / Q000737:chemistry / Q000494:pharmacology*; D013844:Thiazoles / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D051666:Kv1.5 Potassium Channel; D013777:Tetrazoles; D013844:Thiazoles