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

ABSTRACT: 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.

SUBMITTER: Pachon-Angona I

PROVIDER: S-EPMC10819521 | biostudies-literature | 2024 Jan

REPOSITORIES: biostudies-literature

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

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Dataset Information

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

OmicsDI is part of the ELIXIR infrastructure

Tweets

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