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

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, compoun...

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Autores principales: Zhao, Lingyue, Yang, Qian, Tang, Yiqun, You, Qidong, Guo, Xiaoke
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2022
Materias:
Research Paper
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8757610/
https://www.ncbi.nlm.nih.gov/pubmed/35012386
http://dx.doi.org/10.1080/14756366.2021.2018683
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author Zhao, Lingyue
Yang, Qian
Tang, Yiqun
You, Qidong
Guo, Xiaoke
author_facet Zhao, Lingyue
Yang, Qian
Tang, Yiqun
You, Qidong
Guo, Xiaoke
author_sort Zhao, Lingyue
collection PubMed
description 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 (IC(50) = 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.
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spelling pubmed-87576102022-01-14 Design, synthesis, and biological evaluation of arylmethylpiperidines as Kv1.5 potassium channel inhibitors Zhao, Lingyue Yang, Qian Tang, Yiqun You, Qidong Guo, Xiaoke J Enzyme Inhib Med Chem Research Paper 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 (IC(50) = 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. Taylor & Francis 2022-01-10 /pmc/articles/PMC8757610/ /pubmed/35012386 http://dx.doi.org/10.1080/14756366.2021.2018683 Text en © 2022 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. https://creativecommons.org/licenses/by/4.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) ), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Paper
Zhao, Lingyue
Yang, Qian
Tang, Yiqun
You, Qidong
Guo, Xiaoke
Design, synthesis, and biological evaluation of arylmethylpiperidines as Kv1.5 potassium channel inhibitors
title Design, synthesis, and biological evaluation of arylmethylpiperidines as Kv1.5 potassium channel inhibitors
title_full Design, synthesis, and biological evaluation of arylmethylpiperidines as Kv1.5 potassium channel inhibitors
title_fullStr Design, synthesis, and biological evaluation of arylmethylpiperidines as Kv1.5 potassium channel inhibitors
title_full_unstemmed Design, synthesis, and biological evaluation of arylmethylpiperidines as Kv1.5 potassium channel inhibitors
title_short Design, synthesis, and biological evaluation of arylmethylpiperidines as Kv1.5 potassium channel inhibitors
title_sort design, synthesis, and biological evaluation of arylmethylpiperidines as kv1.5 potassium channel inhibitors
topic Research Paper
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8757610/
https://www.ncbi.nlm.nih.gov/pubmed/35012386
http://dx.doi.org/10.1080/14756366.2021.2018683
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