Design and Synthesis of Multi-Functional Ligands through Hantzsch Reaction: Targeting Ca2+ Channels, Activating Nrf2 and Possessing Cathepsin S Inhibitory, and Antioxidant Properties

Autor:	Irene Pachón-Angona, Paul J. Bernard, Alexey Simakov, Maciej Maj, Krzysztof Jozwiak, Anna Novotna, Carina Lemke, Michael Gütschow, Helene Martin, María-Jesús Oset-Gasque, José-Marco Contelles, Lhassane Ismaili
Jazyk:	angličtina
Rok vydání:	2024
Předmět:	calcium channel inhibitors proteases inhibitors antioxidant response element ORAC Alzheimer’s disease Pharmacy and materia medica RS1-441
Zdroj:	Pharmaceutics, Vol 16, Iss 1, p 121 (2024)
Druh dokumentu:	article
ISSN:	1999-4923
DOI:	10.3390/pharmaceutics16010121
Popis:	This work relates to the design and synthesis of a series of novel multi-target directed ligands (MTDLs), i.e., compounds 4a–l, via a convenient one-pot three-component Hantzsch reaction. This approach targeted calcium channel antagonism, antioxidant capacity, cathepsin S inhibition, and interference with Nrf2 transcriptional activation. Of these MTDLs, 4i emerged as a promising compound, demonstrating robust antioxidant activity, the ability to activate Nrf2-ARE pathways, as well as calcium channel blockade and cathepsin S inhibition. Dihydropyridine 4i represents the first example of an MTDL that combines these biological activities.
Databáze:	Directory of Open Access Journals
Externí odkaz:	https://doaj.org/article/91b84aaa929141c3b798a1c55836bddf Zobrazit plný text záznamu View record in DOAJ Plný text ve formátu PDF Plný text ve formátu HTML
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