Design and discovery of Novel Thiazole acetamide derivatives as anticholinesterase agent for possible role in the management of Alzheimer's

Bioorganic & Medicinal Chemistry Letters
Zhi-Qing SunSong-Xia Liu

Abstract

A novel series of thiazole acetamides was synthesized in excellent yields and characterized with the aid of various spectroscopic and elemental analysis. These compounds were evaluated for in vitro acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities for possible benefit in Alzheimers disease (AD). Among the synthesized compound, 6d was identified as the most potent compound of AChE (IC50=3.14±0.16 μM) with a selectivity index (SI) of 2.94 against BuChE. These compounds were further tested for inhibition of Aβ aggregation and β-secretase, where it showed potent inhibition which confirmed its multifactorial benefits in AD. The toxicity and docking study were also carried out to exemplify the pharmacological profile of compound 6d as prospective lead molecule against AD.

References

Sep 27, 2003·Alzheimer Disease and Associated Disorders·Pierre N Tariot
Mar 5, 2011·Lancet·Clive BallardEmma Jones
Aug 20, 2011·Nature Reviews. Drug Discovery·Eric KarranBart De Strooper

❮ Previous
Next ❯

Citations

Sep 20, 2017·Future Medicinal Chemistry·Dawid PanekBarbara Malawska
Feb 23, 2021·Medicinal Chemistry Research : an International Journal for Rapid Communications on Design and Mechanisms of Action of Biologically Active Agents·Haizhou ZhuSwati S More

❮ Previous
Next ❯

Related Concepts

Related Feeds

Alzheimer's Disease: Amyloid Beta

Alzheimer's disease is a neurodegenerative disease associated with the accumulation of amyloid plaques in the brain; these plaques are comprised of amyloid beta deposits. Here is the latest research in this field.