New (benz)imidazolopyridino tacrines as nonhepatotoxic, cholinesterase inhibitors for Alzheimer disease - Archive ouverte HAL Access content directly
Journal Articles Future Medicinal Chemistry Year : 2017

New (benz)imidazolopyridino tacrines as nonhepatotoxic, cholinesterase inhibitors for Alzheimer disease

Houssem Boulebd
  • Function : Author
Helene Martin
  • Function : Author
Alexandre Bonet
  • Function : Author
Mourad Chioua
  • Function : Author
José Marco Contelles
  • Function : Author
Ali Belfaitah

Abstract

Aim: Due to the multifactorial nature of Alzheimer’s disease, there is an urgent search for new more efficient, multitarget-directed drugs. Results: This paper describes the synthesis, antioxidant and in vitro biological evaluation of ten (benz)imidazopyridino tacrines (7–16), showing less toxicity than tacrine at high doses, and potent cholinesterase inhibitory capacity, in the low micromolar range. Among them, compound 10 is a nonhepatotoxic tacrine at 1000 mM, showing moderate, but totally selective electric eel acetylcholinesterase inhibition, whereas molecule 16 is twofold less toxic than tacrine at 1000 μM, showing moderate and almost equipotent inhibition for electric eel acetylcholinesterase and equine butyrylcholinesterase. Conclusion: (Benz)imidazopyridino tacrines (7–16) have been identified as a new and promising type of tacrines for the potential treatment of Alzheimer’s disease.
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Dates and versions

hal-03654691 , version 1 (28-04-2022)

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Houssem Boulebd, Lhassane Ismaili, Helene Martin, Alexandre Bonet, Mourad Chioua, et al.. New (benz)imidazolopyridino tacrines as nonhepatotoxic, cholinesterase inhibitors for Alzheimer disease. Future Medicinal Chemistry, 2017, 9 (8), pp.723-729. ⟨10.4155/fmc-2017-0019⟩. ⟨hal-03654691⟩

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