Synthesis and in vitro assessment of anticholinesterase and antioxidant properties of triazineamide derivatives
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 c...
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Veröffentlicht in: | Future medicinal chemistry 2022-12, Vol.14 (23), p.1741-1753 |
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Hauptverfasser: | , , , , , , , , , |
Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | 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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ISSN: | 1756-8919 1756-8927 |
DOI: | 10.4155/fmc-2022-0200 |