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Updated: Feb 11, 2026

Synthesis and Evaluation of a Ruthenium-based Mitochondrial Calcium Uptake Inhibitor
Published on: October 26, 2017
Design, synthesis and evaluation of substituted piperidine based KCNQ openers as novel antiepileptic agents
Shaoning Yang1, Dingqiang Lu2, Pingkai Ouyang2
1School of Pharmaceutical Sciences, Nanjing University of Technology, Nanjing 211816, PR China; Jiangsu Simcere Pharmaceutical Co. Ltd., Nanjing 210042, PR China.
Abstract:
Epilepsy is a kind of disease with complicated pathogenesis. KCNQ (Kv7) is a voltage dependent potassium channel that is mostly associated with epilepsy and thus becomes an important target in the treatment of epilepsy. In this paper, a series of substituted piperidine derivatives targeting KCNQ were designed and synthesized by using scaffold hopping and active substructure hybridization. Compounds were evaluated by fluorescence-based thallium influx assay, Rb+ flow assay and electrophysiological patch-clamp assay. Results showed that some compounds possessed more potent potassium channel opening activity than Retigabine. More significantly, compound 11 was found to have good pharmacokinetic profiles in vivo.
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