Tacrine based human cholinesterase inhibitors: synthesis of peptidic-tethered derivatives and their effect on potency and selectivity.

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Butini S, Guarino E, Campiani G, Brindisi M, Coccone SS, Fiorini I, Novellino E, Belinskaya T, Saxena A, Gemma S

Tacrine based human cholinesterase inhibitors: synthesis of peptidic-tethered derivatives and their effect on potency and selectivity.

Bioorg Med Chem Lett. 2008 Oct 1;18(19):5213-6. doi: 10.1016/j.bmcl.2008.08.076. Epub 2008 Aug 26.

PubMed ID

18786825 [ View in PubMed

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Abstract

Tacrine based reversible inhibitors of cholinesterases (ChEIs) containing peptidic tethers were synthesized to interact with specific regions at the gorge level, and their potency was determined with human (h) acetylcholinesterase and butyrylcholinesterase. Analogues 3i,j and 3l,m were identified as promising hits and may pave the way for the development of a new series of tacrine based enzyme selective hChEIs.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Tacrine	Acetylcholinesterase	Ki (nM)	36	N/A	N/A	Details