Discovery of an N-(2-aminopyridin-4-ylmethyl) nicotinamide derivative: a potent and orally bioavailable NCX inhibitor

T Kuramochi, A Kakefuda, H Yamada…

文献索引：Kuramochi, Takahiro; Kakefuda, Akio; Yamada, Hiroyoshi; Tsukamoto, Issei; Taguchi, Taku; Sakamoto, Shuichi Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 12 p. 4022 - 4036

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被引用次数: 16

摘要

Ca2+ overload in myocardial cells is responsible for arrhythmia. Sodium–calcium exchanger (NCX) inhibitors are more effective than sodium–hydrogen exchanger (NHE) inhibitors with regard to modulation of Ca2+ overload, because NCX inhibitors can directly inhibit the influx of Ca2+ into cells. NCX is an attractive target for the treatment of heart failure and ischemia- reperfusion. We have designed and synthesized a series of N-(2-aminopyridin-4-ylmethyl) ...