Evaluation of derivatives of 2,3-dihydroquinazolin-4(1H)-one as inhibitors of cholinesterases and their antioxidant activity: In vitro, in silico, and kinetics studies

In search of potent inhibitors of cholinesterase enzymes and antioxidant agents, synthetic derivatives of dihydroquinazolin-4(1H)-one (1?38) were evaluated as potential anti-Alzheimer agents through in vitro acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitions and radical (DPPH a...

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Published in:Journal of the Serbian Chemical Society 2023, Vol.88 (9), p.825-840
Main Authors: Babatunde, Oluwatoyin, Hameed, Shehryar, Mbachu, Kingsley, Saleem, Faiza, Chigurupati, Sridevi, Wadood, Abdul, Ur, Rehman, Venugopal, Vijayan, Khan, Khalid, Taha, Muhammad, Ekundayo, Olusegun, Khan, Maria
Format: Article
Language:English
Subjects:
acetylcholinesterase
antioxidant
butyrylcholinesterase
dual inhibitors
in silico
in vitro
kinetic studies
quinazolinone
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Summary:In search of potent inhibitors of cholinesterase enzymes and antioxidant agents, synthetic derivatives of dihydroquinazolin-4(1H)-one (1?38) were evaluated as potential anti-Alzheimer agents through in vitro acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitions and radical (DPPH and ABTS) scavenging activities. The structure?activity relationship (SAR) was mainly based on the different substituents at the aryl part which showed a significant effect on the inhibitory potential of enzymes and radical scavenging activities. The kinetic studies of most active compounds showed a noncompetitive mode of inhibition for AChE and a competitive mode of inhibition for the BChE enzyme. Additionally, molecular modelling studies were carried out to investigate the possible binding interactions of quinazolinone derivatives with the active site of both enzymes.
ISSN:0352-5139
1820-7421
DOI:10.2298/JSC211106005B