RT Journal Article
T1 Design and Synthesis of Multi-Functional Ligands through Hantzsch Reaction: Targeting Ca2+ Channels, Activating Nrf2 and Possessing Cathepsin S Inhibitory, and Antioxidant Properties
A1 Pachón Angona, Irene
A1 Bernard, Paul J.
A1 Simakov, Alexey
A1 Maj, Maciej
A1 Jozwiak, Krzysztof
A1 Novotna, Anna
A1 Lemke, Carina
A1 Gütschow, Michael
A1 Martin, Helene
A1 Oset Gasque, María Jesús
A1 Contelles, José Marco
A1 Ismaili, Lhassane
AB 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.
PB MDPI
SN 1999-4923
YR 2024
FD 2024-01-17
LK https://hdl.handle.net/20.500.14352/111903
UL https://hdl.handle.net/20.500.14352/111903
LA eng
NO Pachón-Angona, I.; Bernard, P.J.; Simakov, A.; Maj, M.; Jozwiak, K.; Novotna, A.; Lemke, C.; Gütschow, M.; Martin, H.; Oset-Gasque, M.-J.; et al. Design and Synthesis of Multi-Functional Ligands through Hantzsch Reaction: Targeting Ca2+ Channels, Activating Nrf2 and Possessing Cathepsin S Inhibitory, and Antioxidant Properties. Pharmaceutics 2024, 16, 121. https://doi.org/10.3390/pharmaceutics 16010121
NO 2023 Descuento MDPI
DS Docta Complutense
RD 4 may 2025