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Synthesis and  assessment of anticholinesterase and antioxidant properties of triazineamide derivatives. | LitMetric

Cholinesterase inhibitors and radical scavengers have been recognized as powerful symptomatic anti-Alzheimer's disease agents. Hence, the present study aimed to develop new triazineamides as potent anticholinesterase and antioxidant agents. Triazineamide () derivatives were synthesized using cyanuric chloride via nucleophilic substitution followed by condensation. Ellman assay, 2,2-azinobis(3-ethylbenzthiazoline-6-sulfonic acid) radical scavenging assay and molecular docking studies with Autodock 4.2.3 program were conducted. Triazineamide was assessed as a potent, selective and mixed-type dual inhibitor of acetylcholinesterase, with and IC of 5.306 ± 0.002 μM, by binding simultaneously with the catalytic active and peripheral anionic sites of acetylcholinesterase, and it had strong 2,2-azinobis(3-ethylbenzthiazoline-6-sulfonic acid) radical scavenging abilities. These results suggest that triazineamides may be of interest to establish a structural basis for new anti-Alzheimer's disease agents.

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http://dx.doi.org/10.4155/fmc-2022-0200DOI Listing

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