Journal of Medicinal Chemistry p. 880 - 887 (1987)
Update date:2022-08-04
Topics:
Maryanoff, Bruce E.
Nortey, Samuel O.
Gardocki, Joseph F.
Shank, Richard P.
Dodgson, Susanna P.
Novel sugar sulfamate 1 (McN-4853, topiramate) has been found to exhibit potent anticonvulsant activity analogous to that of phenytoin.In the maximal electroshock seizure test, orally at 2 h in mice, 1 had an ED50 of 39 mg/kg.Orally, 1 had a duration of action in excess of 8 h.Other aspects of the pharmacology of 1, as well as neurochemistry and carbonic anhydrase inhibition, are discussed.The conformational behavior of 1 in solution and in the solid state are discussed.A series of analogues of 1 were synthesized and examined for anticonvulsant properties.
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