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

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TitreSynthesis of new Hantzsch adducts showing Ca2+ channel blockade capacity, cholinesterase inhibition and antioxidant power
Type de publicationJournal Article
Year of Publication2021
AuteursPachon-Angona I, Maj M, Wnorowski A, Martin H, Jozwiak K, Ismaili L
JournalFUTURE MEDICINAL CHEMISTRY
Volume13
Date PublishedOCT
Type of ArticleArticle
ISSN1756-8919
Mots-clésAlzheimer's disease, antioxidants, Calcium channel blockers, cholinesterase inhibitors, Hantzsch multicomponent reaction
Résumé

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.

DOI10.4155/fmc-2021-0176