Design,synthesis, and biological evaluation of arylmethylpiperidines as Kv1.5 potassium channel inhibitors |
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| Authors: | Lingyue Zhao Qian Yang Yiqun Tang Qidong You Xiaoke Guo |
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| Institution: | aJiang Su Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing, China;bDepartment of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, China;cDepartment of Clinical Pharmacy, School of Basic Medical Sciences and Clinical Pharmacy, China Pharmaceutical University, Nanjing, China |
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| Abstract: | Kv1.5 potassium channel, encoded by KCNA5, is a promising target for the treatment of atrial fibrillation, one of the common arrhythmia. A new series of arylmethylpiperidines derivatives based on DDO-02001 were synthesised and evaluated for their ability to inhibit Kv1.5 channel. Among them, compound DDO-02005 showed good inhibitory activity (IC50 = 0.72 μM), preferable anti-arrhythmic effects and favoured safety. These results indicate that DDO-02005 can be a promising Kv1.5 inhibitor for further studies.Key Words: Kv1.5 inhibitors, atrial fibrillation, anti-arrhythmia |
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