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Design, synthesis and evaluation of substituted piperidine based KCNQ. openers as novel antiepileptic agents

Epilepsy is a land 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. (C) 2018 Elsevier Ltd. All rights reserved.

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 13925-07-0 help many people in the next few years. Quality Control of 2-Ethyl-3,5-dimethylpyrazine.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem