Voltage-gated sodium channels are attractive therapeutic targets for pain and a number of compounds including Ralfinamide are reported as sodium channel blockers. A new series of vinylpiperidine analog was designed, synthesized and evaluated for ability to block sodium channels. These efforts led to ASP1120 and ASP9596 possessing potent oral analgesic activity on spinal nerve ligation model (Chung model) in rats (ED50 = 2.1 and 0.18 mg/kg, respectively). We describe synthesis, structure-activity relationships and biological properties of vinylpiperidine derivatives. Figure 1. <img src='https://acs-archive-assets2.s3.amazonaws.com/239nm/uploads/2020_10785.jpg' alt='' />

Novel vinylpiperidine derivatives as sodium channel blockers

241st National Meeting (2011)

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