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Wiley-VCH Verlag, ChemInform, 17(37), 2006

DOI: 10.1002/chin.200617169

Elsevier, European Journal of Medicinal Chemistry, 12(40), p. 1222-1245

DOI: 10.1016/j.ejmech.2005.07.009

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

Journal article published in 2005 by Ziad Omran, Jana Sopkova de Oliveira Santos, et A.-L. et A.-L., Thomas Cailly, Elodie Lescot, Jana Sopkova-De Oliveira Santos, Jean-Hugues Agondanou, Vincent Lisowski, Frédéric Fabis, Anne-Marie Godard, Silvia Stiebing, Guillaume Le Flem, Guillaume Le Flem, Michel Boulouard, Patrick Dallemagne ORCID and other authors.
This paper is available in a repository.
This paper is available in a repository.

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Abstract

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 microM) than the reference compound, donepezil (IC50=0.02 microM).