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

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Savini L, Campiani G, Gaeta A, Pellerano C, Fattorusso C, Chiasserini L, Fedorko JM, Saxena A

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

Bioorg Med Chem Lett. 2001 Jul 9;11(13):1779-82.

PubMed ID

11425559 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Tacrine	Acetylcholinesterase	Ki (nM)	40	8	25	Details