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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Bibliographic Details
Published in:	Future medicinal chemistry Vol. 14; no. 23; pp. 1741 - 1753
Main Authors:	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
Format:	Journal Article
Language:	English
Published:	England 01-12-2022
Subjects:	Acetylcholinesterase - metabolism Alzheimer Disease - drug therapy Antioxidants - chemistry Antioxidants - pharmacology Cholinesterase Inhibitors - chemistry Cholinesterase Inhibitors - pharmacology Humans Molecular Docking Simulation Structure-Activity Relationship Sulfonic Acids - chemistry molecular docking cholinesterase Alzheimer's disease ABTS radical scavenging activity
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Summary:	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.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	1756-8919 1756-8927
DOI:	10.4155/fmc-2022-0200