Title of article
Discovery and synthesis of tetrahydroindolone derived semicarbazones as selective Kv1.5 blockers
Author/Authors
Shengde Wu، نويسنده , , Andrew Fluxe، نويسنده , , John M. Janusz، نويسنده , , James B. Sheffer، نويسنده , , R. Greg Browning، نويسنده , , Benjamin Blass، نويسنده , , Keith Cobum، نويسنده , , Richard Hedges، نويسنده , , Michael Murawsky، نويسنده , , Bin Fang، نويسنده , , Gina M. Fadayel، نويسنده , , Michelle Hare، نويسنده , , Laurent Djandjighian، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
5
From page
5859
To page
5863
Abstract
A novel class of tetrahydroindolone-derived semicarbazones has been discovered as potent Kv1.5 blockers. In in vitro studies, several compounds exhibited very good potency for blockade of Kv1.5. Compound 8i showed good selectivity for blockade of Kv1.5 vs hERG and L-type calcium channels. In an anesthetized pig model, compounds 8i and 10c increased atrial ERP about 28%, 18%, respectively, in the right atrium without affecting ventricular ERP.
Keywords
Semicarbazone , Kv1.5 Inhibitor , Atrial antiarrhythmic , In-vivo efficacy
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797490
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