title: Donepezil-ferulic acid hybrids as anti-Alzheimer drugs.
abstract: BACKGROUND
  Due to the complex nature of Alzheimer's disease, there is a renewed and growing search for multitarget drugs.
  
  
  RESULTS
  Donepezil-ferulic acid hybrids (DFAHs) were prepared by the one-pot Ugi-4CR in low-to-moderate yields. DFAHs are potent antioxidant agents, showing oxygen radical absorbance capacity values in the range 4.80-8.71 trolox equivalents, quite higher compared with those recorded for ferulic acid and melatonin. From the ChEs inhibition studies, we conclude that DFAH 8, bearing an ethylene linker, and DFAH 12, bearing a propylene linker, both substituted with a melatonin motif, are the most potent inhibitors, in the nanomolar range.
  
  
  CONCLUSIONS
  We have identified DFAH 8 as a very potent antioxidant, and totally selective equineButyrylCholinEsterase (eqBuChE) inhibitor.
authors.affiliation: NanoMedicine, Imagery & Therapeutics Lab EA 4662, Laboratoire de Chimie Organique et Thérapeutique UFR SMP, CHU Jean Minjoz, Université de Franche-Comté, 19 rue Ambroise Paré, 25030-Besançon, France.
authors.forename: Mohamed
authors.initials: M
authors.lastname: Benchekroun
authors.forename: Lhassane
authors.initials: L
authors.lastname: Ismaili
authors.forename: Marc
authors.initials: M
authors.lastname: Pudlo
authors.forename: Vincent
authors.initials: V
authors.lastname: Luzet
authors.forename: Tijani
authors.initials: T
authors.lastname: Gharbi
authors.forename: Bernard
authors.initials: B
authors.lastname: Refouvelet
authors.forename: José
authors.initials: J
authors.lastname: Marco-Contelles
mesh_terms: D000544:Alzheimer Disease / Q000188:drug therapy*; D000975:Antioxidants / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use*; D002091:Butyrylcholinesterase / Q000737:chemistry / Q000378:metabolism; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use*; D003373:Coumaric Acids / Q000737:chemistry*; D000077265:Donepezil; D006801:Humans; D007189:Indans / Q000737:chemistry*; D010880:Piperidines / Q000737:chemistry*
chemical_list: D000975:Antioxidants; D002800:Cholinesterase Inhibitors; D003373:Coumaric Acids; D007189:Indans; D010880:Piperidines; D000077265:Donepezil; C004999:ferulic acid; D002091:Butyrylcholinesterase