Synthesis and Acetylcholinesterase Inhibitory Assessment of 3-(2-(4-benzoylpiperazin-1-yl) ethylimino) indolin-2-one Derivatives with Potential Anti-Alzheimer Effects
Authors
Abstract
Alzheimer's disease (AD) is a neurodegenerative disorder in geriatric people that characterized by reduction in memory and learning ability. Attenuation of cholinergic system is the most likely hypothesis. Therefore, potentiation of the cholinergic system via inhibition of acetylcholinesterase enzyme could improve and alleviate the symptoms of AD. A new series of isatin-based derivatives (4a-4h) were designed and synthesized according to the pharmacophore of donepezil and consequently related anti-cholinesterase effect was evaluated by Ellman's test. Obtained results were compared with donepezil as a standard drug. All of target derivatives (4a-4h) synthesized with moderate yields. In Ellman's test as an enzymatic assay for acetylcholinesterase, the most of them displayed better inhibitory potency in comparison with donepezil. In summary, isatin-based derivatives could be potential anti-Alzheimer agents. But, more experimental investigations are needed to prove this statement in the future.
Highlights
Copyright
© 2015, Author(s). This open-access article is available under the Creative Commons Attribution 4.0 (CC BY 4.0) International License (https://creativecommons.org/licenses/by/4.0/), which allows for unrestricted use, distribution, and reproduction in any medium, provided that the original work is properly cited.
Similar Articles
Synthesis and Acetylcholinesterase Inhibitory Evaluation of 4-(1,3-Dioxoisoindolin-2-yl)-N-Phenyl Benzamide Derivatives as Potential Anti-Alzheimer Agents
Mohammadi-Farani A, Soltani Darbandi S, Aliabadi A. Synthesis and Acetylcholinesterase Inhibitory Evaluation of 4-(1,3-Dioxoisoindolin-2-yl)-N-Phenyl Benzamide Derivatives as Potential Anti-Alzheimer Agents. Iran J Pharm Res. 2016;15(3):e125144. doi: https://doi.org/10.22037/ijpr.2016.1868
Isatin-Based Anticonvulsant Agents Synthesis and Antiseizure Evaluation in Mice
Rahmani Khajouei M, Mohammadi-Farani A, Mirzaei D, Aliabadi A. Isatin-Based Anticonvulsant Agents Synthesis and Antiseizure Evaluation in Mice. J Rep Pharm Sci. 2017;6(1):e147618. doi:
Synthesis, docking and acetylcholinesterase inhibitory evaluation of (E)-3-(4-(diethylamino) phenyl)-1-phenylprop- 2-en-1-one derivatives with probable anti-Alzheimer effects
Aliabadi A, Mohammadi-Farani A, Ahmadvand MJ, Rahmani Khajouei M. Synthesis, docking and acetylcholinesterase inhibitory evaluation of (E)-3-(4-(diethylamino) phenyl)-1-phenylprop- 2-en-1-one derivatives with probable anti-Alzheimer effects. J Rep Pharm Sci. 2017;6(2):e147611. doi:
Design, Synthesis, Molecular Dynamics Analysis, and Biological Evaluation of New Urea Derivatives in an Animal Model of Alzheimer Disease
Heidarian S, Faizi M, Alemi M, Garmabdari A, Nikray N, et al. Design, Synthesis, Molecular Dynamics Analysis, and Biological Evaluation of New Urea Derivatives in an Animal Model of Alzheimer Disease. Iran J Pharm Res. 2026;25(1):e172672. doi: https://doi.org/10.5812/ijpr-172672
Synthesis and Antimicrobial Activity of Some New Isatin Derivatives
Patel A, Bari S, Talele G, Patel J, Sarangapani M. Synthesis and Antimicrobial Activity of Some New Isatin Derivatives. Iran J Pharm Res. 2022;5(4):e128295. doi: https://doi.org/10.22037/ijpr.2010.685
- Scopus by DOI: 0
Last Update: 1 week ago
- Scopus by Title: 11
Last Update: 1 week ago
- Scopus by Title (Ref): 14
Last Update: 1 week ago
- CrossRef: 0
Last Update: 5 hours ago
- OpenAlex: 0
Last Update: 7 hours ago
- OpenCitations: 0
Last Update: 5 days ago