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Synthesis of new Hantzsch adducts showing Ca 2+ channel blockade capacity, cholinesterase inhibition and antioxidant power

Abstract : 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 Ca 2+ channel blockade capacity, cholinesterase inhibition and antioxidant power. Results: Compound 4l showed submicromolar inhibition of butyrylcholinesterase, Ca 2+ 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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https://hal-univ-fcomte.archives-ouvertes.fr/hal-03654559
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Submitted on : Thursday, April 28, 2022 - 4:41:42 PM
Last modification on : Friday, April 29, 2022 - 3:08:35 AM

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Irene Pachón-Angona, Maciej Maj, Artur Wnorowski, Helene Martin, Krzysztof Jóźwiak, et al.. Synthesis of new Hantzsch adducts showing Ca 2+ channel blockade capacity, cholinesterase inhibition and antioxidant power. Future Medicinal Chemistry, Future Science, 2021, 13 (20), pp.1717-1729. ⟨10.4155/fmc-2021-0176⟩. ⟨hal-03654559⟩

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