Discovery and in vitro/in vivo studies of tetrazole derivatives as Kv1. 5 blockers

…, R White, C Jackson, R Hedges, M Murawsky…

文献索引：Wu, Shengde; Fluxe, Andrew; Sheffer, Jim; Janusz, John M.; Blass, Benjamin E.; White, Ron; Jackson, Chris; Hedges, Richard; Murawsky, Michael; Fang, Bin; Fadayel, Gina M.; Hare, Michelle; Djandjighian, Laurent Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 24 p. 6213 - 6218

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被引用次数: 39

摘要

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. ... A novel class of tetrazole-derived Kv1.5 blockers is disclosed. In in vitro studies, several compounds had IC 50 ranging from 180 to 550 nM. In vivo studies indicated that compounds 2f and 2j increased right atrial ERP ...