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-Reference-Cited by-同舟云学术

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

Published:2023 Issue:9 Volume:88 Page:825-840
ISSN:0352-5139
Container-title:Journal of the Serbian Chemical Society
language:en
Short-container-title:JSCS

Author:

Babatunde Oluwatoyin¹^ORCID,Hameed Shehryar¹^ORCID,Mbachu Kingsley²,Saleem Faiza¹^ORCID,Chigurupati Sridevi³,Wadood Abdul⁴,Ur Rehman⁴^ORCID,Venugopal Vijayan⁵^ORCID,Khan Khalid⁶^ORCID,Taha Muhammad⁷,Ekundayo Olusegun⁸^ORCID,Khan Maria⁹^ORCID

Affiliation:

1. H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan

2. H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan + Department of Chemistry, University of Ibadan, Nigeria

3. Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, Qassim University, Buraydah, Saudi Arabia

4. Department of Biochemistry, Computational Medicinal Chemistry Laboratory, UCSS, Abdul Wali Khan University, Mardan, Pakistan

5. Faculty of Pharmacy, AIMST University, Kedah, Malaysia

6. H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan + Department of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, Dammam, Saudi Arabia

7. Department of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, Dammam, Saudi Arabia

8. Department of Chemistry, University of Ibadan, Nigeria

9. Third World Center for Science and Technology, H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan

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.

Publisher

National Library of Serbia

Subject

General Chemistry

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