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ID: ALA4118146
Journal: Bioorg Med Chem Lett
Title: Design, synthesis and evaluation of substituted piperidine based KCNQ openers as novel antiepileptic agents.
Authors: Yang S, Lu D, Ouyang P.
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.
CiteXplore: 29706422