Riluzole series. Synthesis and in vivo “antiglutamate” activity of 6-substituted-2-benzothiazolamines and 3-substituted-2-imino-benzothiazolines

…, M Barreau, JC Blanchard, A Boireau…

Index: Jimonet, Patrick; Audiau, Francois; Barreau, Michel; Blanchard, Jean-Charles; Boireau, Alain; Bour, Yvette; Coleno, Marie-Annick; Doble, Adam; Doerflinger, Gilles; Do Huu, Claudine; Donat, Marie-Helene; Duchesne, Jean Marie; Ganil, Pierre; Gueremy, Claude; Honore, Eliane; Just, Bernard; Kerphirique, Roselyne; Gontier, Sylvie; Hubert, Philippe; Laduron, Pierre M.; Blevec, Joseph Le; Meunier, Mireille; Miquet, Jean-Marie; Nemecek, Conception; Pasquet, Martine; Piot, Odile; Pratt, Jeremy; Rataud, Jean; Reibaud, Michel; Stutzmann, Jean-Marie; Mignani, Serge Journal of Medicinal Chemistry, 1999 , vol. 42, # 15 p. 2828 - 2843

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Citation Number: 178

Abstract

Two series of analogues of riluzole, a blocker of excitatory amino acid mediated neurotransmission, have been synthesized: monosubstituted 2-benzothiazolamines and 3- substituted derivatives. Of all the compounds prepared in the first series, only 2- benzothiazolamines bearing alkyl, polyfluoroalkyl, or polyfluoroalkoxy substituents in the 6- position showed potent anticonvulsant activity against administration of glutamic acid in ...