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

Author:

Pachón-Angona Irene12,Maj Maciej3ORCID,Wnorowski Artur3ORCID,Martin Helene4,Jóźwiak Krzysztof3ORCID,Ismaili Lhassane1ORCID

Affiliation:

1. Neurosciences intégratives et cliniques EA 481, Pôle de Chimie Organique et Thérapeutique, Univ. Bourgogne Franche-Comté, UFR Santé, 19, rue Ambroise Paré, Besançon, F-25000, France

2. Current address: Engineering & Medicine for Human Health (ChEM-H), Stanford University, Stanford, CA 94305, USA

3. Department of Biopharmacy, Medical University of Lublin, ul. W. Chodzki 4a, Lublin, 20-093, Poland

4. PEPITE EA4267, Laboratoire de Toxicologie Cellulaire, Univ. Bourgogne Franche-Comté, Besançon, F-25000, France

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 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.

Funder

Regional Council of Franche-Comté

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

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3. Synthesis, Characterization, and Inhibition Study of Novel Substituted Phenylureido Sulfaguanidine Derivatives as α‐Glycosidase and Cholinesterase Inhibitors

4. Alzheimer's disease

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