Synthesis and biological evaluation as AChE inhibitors of new indanones and thiaindanones related to donepezil

DOI: 10.1016/j.ejmech.2005.07.009

Source and publish data:

European Journal of Medicinal Chemistry p. 1222 - 1245 (2005)

Update date:2022-08-02

Topics:

Authors:

Omran, Ziad

Cailly, Thomas

Lescot, Elodie

Santos, Jana Sopkova-De Oliveira

Agondanou, Jean-Hugues

Lisowski, Vincent

Fabis, Frederic

Godard, Anne-Marie

Stiebing, Silvia

Le Flem, Guillaume

Boulouard, Michel

Dauphin, Francois

Dallemagne, Patrick

Rault, Sylvain

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Article abstract of DOI:10.1016/j.ejmech.2005.07.009

Sixty-four new indanones and thiaindanones related to donepezil were synthesized and evaluated in vitro as potential AChE inhibitors. Among them, 11 derivatives were found to inhibit the enzyme in the submicromolar range; the best compound revealed its inhibitory activity with an IC₅₀ in the same range (0.06 μM) than the reference compound, donepezil (IC₅₀ = 0.02 μM).

Full text of DOI:10.1016/j.ejmech.2005.07.009

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