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Anticonvulsant sugar sulfamates. Potent cyclic sulfate and cyclic sulfite analogues of topiramate |
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| Authors: | Bruce E. Maryanoff Michael J. Costanzo Ricahrd P. Shank James J. Schupsky Marta E. Ortegon Jeffry L. Vaught |
| Affiliation: | a Departments of Medicinial Chemistry, The R. W. Johnson Pharmaceutical Research Institute Spring House, Pennsylvania 19477 USA b Department of CNS Research, The R. W. Johnson Pharmaceutical Research Institute Spring House, Pennsylvania 19477 USA |
| Abstract: | Exploration structure-activity relationships surrounding the clinically effective antiepileptic drug topiramate (1) led to a series of potent anticonvulsants with a 4,5-cyclic sulfate or 4,5-cycli sulfite functionality. Key derivative 2 (RWJ-37947) is ca. 8 times more potent than topiramate in mice; it also features a long duration of action and a very favorable neurotoxicity index. |
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