학술논문
Design and Synthesis of Multi-Functional Ligands through Hantzsch Reaction: Targeting Ca 2+ Channels, Activating Nrf2 and Possessing Cathepsin S Inhibitory, and Antioxidant Properties.
Document Type
Article
Author
Source
Subject
*CALCIUM ions
*CALCIUM channels
*NUCLEAR factor E2 related factor
*LIGANDS (Biochemistry)
*OXIDANT status
*ANTIOXIDANTS
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Language
ISSN
1999-4923
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. [ABSTRACT FROM AUTHOR]