Design, synthesis, and biological evaluation of arylmethylpiperidines as Kv1.5 potassium channel inhibitors. (31st December 2022)

• Record Type: Journal Article
• Authors: Zhao, Lingyue; Yang, Qian; Tang, Yiqun; You, Qidong; Guo, Xiaoke
• Is Part Of: Journal of enzyme inhibition and medicinal chemistry. Volume 37:Number 1(2022)
• Page Start: 462
• Page End: 471
• Publication Date: 2022-12-31
• Subjects: Kv1.5 inhibitors -- atrial fibrillation -- anti-arrhythmia; Enzyme inhibitors -- Periodicals; Enzyme Inhibitors -- periodicals; Biochemistry -- periodicals; 572.7
• DOI: 10.1080/14756366.2021.2018683
• Languages: English
• ISSNs: 1475-6366

Abstract

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. Graphical abstract: UF0001