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Novel indanone-chalcone esters with potential anti-Alzheimer effects designed using hybridization and bioisosteric replacement approaches by Fereshteh Azimian; Mohammad Shahrivar-Gargari; Teymour Vahedpour; Salar Hemmati; Mahrokh Dastmalchi; Tuba Tüylü Küçükkılınç; Siavoush Dastmalchi is a Chemistry article available to read on EtoBox.
What is Novel indanone-chalcone esters with potential anti-Alzheimer effects designed using hybridization and bioisosteric replacement approaches about?
Using molecular hybridization and bioisosteric replacement approaches, novel agents with potential use for the treatment of Alzheimer's disease (AD) were developed based on the structure of donepezil. A series of 14 indanone-chalcones bearing ester group were designed, synthesized, and then characterized using variety of methods. All target compounds showed moderate acetylcholinesterase (AChE) inhibitory potencies and among them, the most active compound 8e exhibited inhibitory activity with IC 50 value of 18.7 μM against AChE. Also, Aβ 1-40 aggregation inhibitory activities of the synthesized compounds were evaluated, and the results showed that compound 8h was able to inhibit Aβ 1-40 aggregation by 81.6%. The results of docking studies revealed that some of compounds fits well into the binding site of AChE. The most active AChE inhibiting derivative 8e has close physico-chemical properties to donepezil (reference compound) and passed more drug likeness filters relative to the reference compound. Collectively, the current study provides insight for designing drug size molecules with ester group to target acetylcholinesterase in the process of developing new active compounds for AD
Who reads Novel indanone-chalcone esters with potential anti-Alzheimer effects designed using hybridization and bioisosteric replacement approaches?
It is typically read by researchers, students, and practitioners in Chemistry.
- Author
- Fereshteh Azimian; Mohammad Shahrivar-Gargari; Teymour Vahedpour; Salar Hemmati; Mahrokh Dastmalchi; Tuba Tüylü Küçükkılınç; Siavoush Dastmalchi
- Publisher
- Springer Science and Business Media LLC
- Published
- 2023
- Language
- EN
- Field
- Chemistry (Physical Sciences)