Il Farmaco

Design, synthesis and biological evaluation of ambenonium derivatives as AChE inhibitors

ML Bolognesi, A Cavalli, V Andrisano, M Bartolini…

Index: Bolognesi, Maria Laura; Cavalli, Andrea; Andrisano, Vincenza; Bartolini, Manuela; Banzi, Rita; Antonello, Alessandra; Rosini, Michela; Melchiorre, Carlo Farmaco, 2003 , vol. 58, # 9 p. 917 - 928

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Citation Number: 10

Abstract

Ambenonium (1), an old AChE inhibitor, is endowed with an outstanding affinity and a peculiar mechanism of action that, taken together, make it a very promising pharmacological tool for the treatment of Alzheimer's disease (AD). Unfortunately, the bisquaternary structure of 1 prevents its passage through the blood brain barrier. In a search of centrally active ambenonium derivatives, we planned to synthesize tertiary amines of 1, such as 2 and 3. ...