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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.
- Source :
-
Journal of the Serbian Chemical Society . 2023, Vol. 88 Issue 9, p825-840. 16p. - Publication Year :
- 2023
-
Abstract
- 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. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 03525139
- Volume :
- 88
- Issue :
- 9
- Database :
- Academic Search Index
- Journal :
- Journal of the Serbian Chemical Society
- Publication Type :
- Academic Journal
- Accession number :
- 173260439
- Full Text :
- https://doi.org/10.2298/JSC211106005B