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
Hauptverfasser: Vatturu, Murali, Rao, Kandrakonda Yelamanda, Yesu, Valaparla Bala, Basha, Shaik Jeelan, Guptha, Tanguturi Prakash, Babu, Donka Suresh, Sajitha, Kethineni, Kalyan, Gundlapalli Pavan, Damu, Amooru Gangaiah, Srinivasulu, Doddaga
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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.
ISSN:1756-8919
1756-8927
DOI:10.4155/fmc-2022-0200