Design, synthesis, and biological evaluation of arylmethylpiperidines as Kv1.5 potassium channel inhibitors.

J Enzyme Inhib Med Chem

Jiang Su Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing, China.

Published: December 2022

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 were synthesised and evaluated for their ability to inhibit Kv1.5 channel. Among them, compound showed good inhibitory activity (IC = 0.72 μM), preferable anti-arrhythmic effects and favoured safety. These results indicate that can be a promising Kv1.5 inhibitor for further studies.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8757610PMC
http://dx.doi.org/10.1080/14756366.2021.2018683DOI Listing

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