Novel carvedilol analogues that suppress store-overload-induced Ca2+ release

CD Smith, A Wang, K Vembaiyan, J Zhang…

文献索引：Smith, Chris D.; Wang, Aixia; Vembaiyan, Kannan; Zhang, Jingqun; Xie, Cuihong; Zhou, Qiang; Wu, Guogen; Chen, S. R. Wayne; Back, Thomas G. Journal of Medicinal Chemistry, 2013 , vol. 56, # 21 p. 8626 - 8655

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被引用次数: 9

摘要

Carvedilol is a uniquely effective drug for the treatment of cardiac arrhythmias in patients with heart failure. This activity is in part because of its ability to inhibit store-overload-induced calcium release (SOICR) through the RyR2 channel. We describe the synthesis, characterization, and bioassay of ca. 100 compounds based on the carvedilol motif to identify features that correlate with and optimize SOICR inhibition. A single-cell bioassay ...