| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10591518 | Bioorganic & Medicinal Chemistry Letters | 2013 | 5 Pages |
Abstract
A novel series of pyrrolidine derivatives as Na+ channel blockers was synthesized and evaluated for their inhibitory effects on neuronal Na+ channels. Structure-activity relationship (SAR) studies of a pyrrolidine analogue 2 led to the discovery of 5e as a potent Na+ channel blocker with a low inhibitory action against human ether-a-go-go-related gene (hERG) channels. Compound 5e showed remarkably neuroprotective activity in a rat transient middle cerebral artery occlusion (MCAO) model, suggesting that 5e would act as a neuroprotectant for ischemic stroke.
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Authors
Maki Seki, Osamu Tsuruta, Ryo Tatsumi, Aki Soejima,