Novel and potent tacrine-related hetero-and homobivalent ligands for acetylcholinesterase and butyrylcholinesterase

L Savini, G Campiani, A Gaeta, C Pellerano…

Index: Savini, Luisa; Campiani, Giuseppe; Gaeta, Alessandra; Pellerano, Cesare; Fattorusso, Caterina; Chiasserini, Luisa; Fedorko, James M.; Saxena, Ashima Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 13 p. 1779 - 1782

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Citation Number: 50

Abstract

Based upon synthetic and biochemical results, a novel and potent tacrine analogue and heterobivalent analogues of tacrine, were designed. The role played by the amino groups of homo-and heterobivalent ligands in the interaction with the peripheral and catalytic sites of AChE and BuChE were investigated. The syntheses of these materials together with the results of AChE/BuChE inhibition assays are detailed.