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Published:
Feb 11, 2025Keywords:
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Main Article Content
Synthesis and biological activities of novel spiroquinazoline derivatives for Alzheimer’s disease
Abstract
Purpose: To synthesize novel spiroquinazoline derivatives and determine their biological properties as
acetylcholinesterase (AChE) inhibitors and antioxidant agents.
Methods: Several quinazoline derivatives (3-5) were synthesized using N-methylisatoic anhydride (1)
as starting material. Synthesized compounds were fully characterized using thin-layer chromatography
(TLC), mass spectroscopy (MS) and nuclear magnetic resonance (NMR) techniques. Furthermore, in
vitro anticholinesterase and antioxidant activities of compound 5 were determined using Ellman’s and
1,1-diphenyl 2-picrylhydrazyl (DPPH) assays, respectively.
Results: The synthesis resulted in a good yield of compound 5 (71 %), which demonstrated potent
inhibitory effect on acetylcholinesterase enzyme (IC50 = 11.89 μmol/mL) and significant antioxidant
activity (IC50 = 143.7 μmol/mL).
Conclusion: The synthesized spiroquinazoline derivative 5 exhibits very good anti-AChE
anticholinesterase and antioxidant activities. Thus, it has potential for further development for use in
Alzheimer's disease (AD) therapy. Future studies are required to elucidate whether compound 5 has
direct effects on Tau aggregation or Aβ production and to investigate its full therapeutic potential in the
context of these predominant AD hypotheses.
