4.5 Article

Synthesis of new Hantzsch adducts showing Ca2+ channel blockade capacity, cholinesterase inhibition and antioxidant power

Journal

FUTURE MEDICINAL CHEMISTRY
Volume 13, Issue 20, Pages -

Publisher

FUTURE SCI LTD
DOI: 10.4155/fmc-2021-0176

Keywords

Alzheimer's disease; antioxidants; calcium channel blockers; cholinesterase inhibitors; Hantzsch multicomponent reaction

Funding

  1. Regional Council of Franche-Comte PRIME [2016YC-04540, 04560]

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This study synthesized twelve new compounds and evaluated their Ca2+ channel blockade capacity, cholinesterase inhibition, and antioxidant power. Results showed that one of the compounds has the potential for Alzheimer's disease therapy.
Background: Alzheimer's disease is a chronic neurodegenerative chronic disease with a heavy social and economic impact in our developed societies, which still lacks an efficient therapy. Method: This paper describes the Hantzsch multicomponent synthesis of twelve alkyl hexahydro-quinoline-3-carboxylates, 4a-l, along with the evaluation of their Ca2+ channel blockade capacity, cholinesterase inhibition and antioxidant power. Results: Compound 4l showed submicromolar inhibition of butyrylcholinesterase, Ca2+ channel antagonism and an antioxidant effect. Conclusion: Compound 4l is an interesting compound that deserves further investigation for Alzheimer's disease therapy.

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