1,4-Disubstituted Piperazin-2-Ones as Selective Late Sodium Current Inhibitors with QT Interval Shortening Properties in Isolated Rabbit Hearts
Hui Yang,
Mengqin Jing,
Chao Tian
et al.
Abstract:Late sodium current (I Na ) inhibitors are a new subclass of antiarrhythmic agents. To overcome the drawbacks, e.g., low efficacy and inhibition effect on K + current, of the FDAapproved late I Na inhibitor ranolazine, chain amide 6a−6q, 1,4disubstituted piperazin-2-ones 7a−7s, and their derivatives 8a−8n were successively designed, synthesized, and evaluated in vitro on the Na V 1.5-transfected HEK293T cells by the whole-cell patch clamp recording assay at the concentration of 40 μM. Among the new skeleton co… Show more
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