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Lactam sulfonamides as potent inhibitors of the Kv1.5 potassium ion channel |
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| Institution: | 2. Institute of Neurobiology, Bulgarian Academy of Sciences, Sofia, Bulgaria;1. Institute of Chemistry, Saint Petersburg State University, Universitetskiy Pr., 26, 198504 Saint Petersburg, Russian Federation;2. Institute of Macromolecular Compounds of Russian Academy of Sciences, V.O. Bolshoi Pr. 31, 199004 Saint Petersburg, Russian Federation |
| Abstract: | A series of lactam sulfonamides has been discovered and optimized as inhibitors of the Kv1.5 potassium ion channel for treatment of atrial fibrillation. In vitro structure–activity relationships from lead structure C to optimized structure 3y are described. Compound 3y was evaluated in a rabbit PD-model and was found to selectively prolong the atrial effective refractory period at submicromolar concentrations. |
| Keywords: | Atrial fibrillation Kv1 5 IKur Lactams Sulfonamides |
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