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Design, Synthesis, Biological Activity, and Molecular Modeling of Novel Spiroquinazoline Derivatives as Acetylcholinesterase Inhibitors for Alzheimer Disease.
- Source :
-
Polycyclic Aromatic Compounds . 2023, Vol. 43 Issue 9, p8082-8095. 14p. - Publication Year :
- 2023
-
Abstract
- The p-toluene sulfonic acid (p-TSA) catalyzed cascade ring closing transformation has been executed for the preparation of novel spiroquinazolinone compounds 4 and 5 by the reaction between anthranilamide and cyclohexanone followed by subsequent acylation. These molecules were then examined against the inhibitory activity of Acetylcholineterase (AchE). The tested compounds revealed moderate anti-AChE activity of IC50 values ranging from 46.675 to 14.256 µM). The described results lead toward the development of compounds 4b and 5c having promising anti-AChE activities with IC50 values at the micromolar level. The docking study suggests that these hybrid spiroquinazolinone scaffold might facilitate the further development of investigated compounds as anti-Alzheimer agents. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 10406638
- Volume :
- 43
- Issue :
- 9
- Database :
- Academic Search Index
- Journal :
- Polycyclic Aromatic Compounds
- Publication Type :
- Academic Journal
- Accession number :
- 173321527
- Full Text :
- https://doi.org/10.1080/10406638.2022.2144911