AI Article Synopsis
- Nineteen new thiazole-based compounds were synthesized and characterized using analytical and spectral methods.
- Two compounds demonstrated strong acetylcholinesterase (AChE) inhibitory activity with IC values of 103.24 and 108.94 nM.
- Another set of compounds showed moderate activity, and molecular docking studies indicated that these active compounds bind similarly to donepezil, suggesting their potential as new AChE inhibitors.
Article Abstract
Nineteen new thiazole-based derivatives were synthesized and their structures characterized with analytical and spectral data. The assessment of their acetylcholinesterase (AChE) inhibitory activity revealed that compounds and produced potent AChE inhibitory activities with IC values of 103.24 and 108.94 nM, respectively. Compounds , , , , , , and displayed moderate activity with 25-50% relative potency compared to the known potent AChE inhibitor donepezil. Molecular docking studies of the active compounds docked within the active site cavity of AChE showed a binding orientation similar to that of donepezil, with good predicted binding affinities. These compounds could therefore be considered as potential lead compounds for the development of new and potentially improved AChE inhibitors.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8320107 | PMC |
| http://dx.doi.org/10.1021/acsomega.1c02549 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!