期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 5, 页码 1477-1480出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.01.022
关键词
Arrhythmia; Class III anti-arrhythmic agents; I-Kr and I-Ks dual blockers; Molecular hybridization
资金
- China National 863 Program [2007AA02Z307]
- Innovation Program for the Postgraduates in Jiangsu
The combination of I-Kr and I-Ks blockade could lead to synergistic and safe class III anti-arrhythmic effect with the enhanced efficacy and reduced risk. On the rationale of structural hybridization of azimilide and HMR-1556, a novel series of IKr and IKs dual blockers were designed, synthesized and evaluated in vitro. One compound, 3r (CPUY11018), deserves further evaluation for its potent anti-arrhythmic activity and favorable cardiovascular profile. (C) 2009 Elsevier Ltd. All rights reserved.
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