1121057-69-9Relevant articles and documents
Design, synthesis and evaluation of substituted piperidine based KCNQ openers as novel antiepileptic agents
Yang, Shaoning,Lu, Dingqiang,Ouyang, Pingkai
supporting information, p. 1731 - 1735 (2018/05/04)
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.