4,10-Dihydro-4-oxo-4 H -imidazo[1,2- a ]indeno[1,2- e ]pyrazin-2-carboxylic acid derivatives
作者:Jean-Marie Stutzmann、Georg Andrees Bohme、Alain Boireau、Dominique Damour、Marc Williams Debono、Arielle Genevois-Borella、Assunta Imperato、Patrick Jimonet、Jeremy Pratt、John C.R. Randle、Yves Ribeill、Marc Vuilhorgne、Serge Mignani
DOI:10.1016/s0960-894x(00)00181-5
日期:2000.5
A novel series of 2-substituted-4,5-dihydro-4-oxo-4H-imidazo[1,2-a]indeno[1,2-e]pyrazine derivatives was synthesised. One of them, 4e-a highly water soluble compound - exhibited a nanomolar affinity and demonstrated competitive antagonist properties at the ionotropic AMPA receptors. This compound also displayed potent anticonvulsant properties against electrically or sound-induced convulsions in mice after systemic administration, thus suggesting adequate brain penetration. (C) 2000 Elsevier Science Ltd. All rights reserved.