title: Synthesis and biological evaluation as AChE inhibitors of new indanones and thiaindanones related to donepezil.
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).
authors.affiliation: Centre d'études et de recherche sur le médicament de Normandie, département de pharmacochimie U.F.R. des sciences pharmaceutiques, université de Caen Basse-Normandie, boulevard Becquerel, 14032 Caen cedex, France.
authors.forename: Ziad
authors.initials: Z
authors.lastname: Omran
authors.forename: Thomas
authors.initials: T
authors.lastname: Cailly
authors.forename: Elodie
authors.initials: E
authors.lastname: Lescot
authors.forename: Jana Sopkova-de Oliveira
authors.initials: JS
authors.lastname: Santos
authors.forename: Jean-Hugues
authors.initials: JH
authors.lastname: Agondanou
authors.forename: Vincent
authors.initials: V
authors.lastname: Lisowski
authors.forename: Frédéric
authors.initials: F
authors.lastname: Fabis
authors.forename: Anne-Marie
authors.initials: AM
authors.lastname: Godard
authors.forename: Silvia
authors.initials: S
authors.lastname: Stiebing
authors.forename: Guillaume
authors.initials: G
authors.lastname: Le Flem
authors.forename: Michel
authors.initials: M
authors.lastname: Boulouard
authors.forename: François
authors.initials: F
authors.lastname: Dauphin
authors.forename: Patrick
authors.initials: P
authors.lastname: Dallemagne
authors.forename: Sylvain
authors.initials: S
authors.lastname: Rault
mesh_terms: D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D018360:Crystallography, X-Ray; D000077265:Donepezil; D015195:Drug Design; D007189:Indans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008958:Models, Molecular; D015394:Molecular Structure; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D002800:Cholinesterase Inhibitors; D007189:Indans; D010880:Piperidines; D000077265:Donepezil