2. Academic Validation
  3. Design, synthesis, and biological evaluation of arylmethylpiperidines as Kv1.5 potassium channel inhibitors

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

  • J Enzyme Inhib Med Chem. 2022 Dec;37(1):462-471. doi: 10.1080/14756366.2021.2018683.
Lingyue Zhao 1 2,  Qian Yang 1 2,  Yiqun Tang 3,  Qidong You 1 2,  Xiaoke Guo 1 2
Affiliations

Affiliations

  • 1 Jiang Su Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing, China.
  • 2 Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing, China.
  • 3 Department of Clinical Pharmacy, School of Basic Medical Sciences and Clinical Pharmacy, China Pharmaceutical University, Nanjing, China.
PMID: 35012386 DOI: 10.1080/14756366.2021.2018683
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.

Keywords

Kv1.5 inhibitors; anti-arrhythmia; atrial fibrillation.

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