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
| Autor: | Babatunde Oluwatoyin, Hameed Shehryar, Mbachu Kingsley Adibe, Saleem Faiza, Chigurupati Sridevi, Wadood Abdul, Ur Rehman Ashfaq, Venugopal Vijayan, Khan Khalid Mohammed, Taha Muhammad, Ekundayo Olusegun, Khan Maria Aqeel |
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| Jazyk: | angličtina |
| Rok vydání: | 2023 |
| Předmět: | |
| Zdroj: | Journal of the Serbian Chemical Society, Vol 88, Iss 9, Pp 825-840 (2023) |
| Druh dokumentu: | article |
| ISSN: | 0352-5139 1820-7421 |
| DOI: | 10.2298/JSC211106005B |
| Popis: | 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. |
| Databáze: | Directory of Open Access Journals |
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