Anticonvulsant sugar sulfamates. Potent cyclic sulfate and cyclic sulfite analogues of topiramate

Bioorganic & Medicinal Chemistry Letters
1993.0

Abstract

Exploration of 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-cyclic 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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