Literature DB >> 16137794

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

Ziad Omran1, Thomas Cailly, Elodie Lescot, Jana Sopkova-de Oliveira Santos, Jean-Hugues Agondanou, Vincent Lisowski, Frédéric Fabis, Anne-Marie Godard, Silvia Stiebing, Guillaume Le Flem, Michel Boulouard, François Dauphin, Patrick Dallemagne, Sylvain Rault.   

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).

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Year:  2005        PMID: 16137794     DOI: 10.1016/j.ejmech.2005.07.009

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  1 in total

1.  Synthesis and biological evaluation of thiophene derivatives as acetylcholinesterase inhibitors.

Authors:  Mohamed M Ismail; Mona M Kamel; Lamia W Mohamed; Samar I Faggal; Mai A Galal
Journal:  Molecules       Date:  2012-06-12       Impact factor: 4.411

  1 in total

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