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: | Oluwatoyin Babatunde, Shehryar Hameed, Kingsley Mbachu, Faiza Saleem, Sridevi Chigurupati, Abdul Wadood, Rehman Ur, Vijayan Venugopal, Khalid Khan, Muhammad Taha, Olusegun Ekundayo, Maria Khan |
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| Rok vydání: | 2023 |
| Předmět: | |
| Zdroj: | Journal of the Serbian Chemical Society. :5-5 |
| ISSN: | 1820-7421 0352-5139 |
| Popis: | In search of potent inhibitors of cholinesterase enzymes and antioxidant agents, synthetic derivatives 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 (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 modeling studies were carried out to investigate the possible binding interactions of quinazolinone derivatives with the active site of both enzymes. |
| Databáze: | OpenAIRE |
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