Novel and potent tacrine-related hetero- and homobivalent ligands for acetylcholinesterase and butyrylcholinesterase.
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.
Savini
L
L
Dipartimento Farmaco Chimico Tecnologico, Università degli Studi di Siena, via Aldo Moro, 53100, Siena, Italy. svaini@unisi.it
Campiani
G
G
Gaeta
A
A
Pellerano
C
C
Fattorusso
C
C
Chiasserini
L
L
Fedorko
J M
JM
Saxena
A
A
D000110:Acetylcholinesterase / Q000737:chemistry / Q000378:metabolism*; D002091:Butyrylcholinesterase / Q000737:chemistry / Q000378:metabolism*; D020134:Catalytic Domain; D008024:Ligands; D013619:Tacrine / Q000737:chemistry / Q000378:metabolism*
D008024:Ligands; D013619:Tacrine; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase