Discovery of 4-substituted pyrrolidone butanamides as new agents with significant antiepileptic activity

…, PM Pasau, E Differding, BI Lallemand…

Index: Kenda, Benoit M.; Matagne, Alain C.; Talaga, Patrice E.; Pasau, Patrick M.; Differding, Edmond; Lallemand, Benedicte I.; Frycia, Anne M.; Moureau, Florence G.; Klitgaard, Henrik V.; Gillard, Michel R.; Fuks, Bruno; Michel, Philippe Journal of Medicinal Chemistry, 2004 , vol. 47, # 3 p. 530 - 549

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Citation Number: 155

Abstract

(S)-α-ethyl-2-oxopyrrolidine acetamide 2 (levetiracetam, Keppra, UCB SA), a structural analogue of piracetam, has recently been approved as an add-on treatment of refractory partial onset seizures in adults. This drug appears to combine significant efficacy and high tolerability due to a unique mechanism of action. The latter relates to a brain-specific binding site for 2 (LBS for levetiracetam binding site) that probably plays a major role in its ...