Hybrids of Methylxanthines and Azoderivatives as Acetylcholinesterase Inhibitors: Structure–Activity Relationship Analysis
In this work, we synthesized methylxanthine and azobenzene derivatives, linked to secondary amines via a seven-carbon chain, to evaluate their acetylcholinesterase (AChE) inhibitory activity. Among the azobenzene compounds, <b>3a</b> exhibited the highest activity with an IC<sub>50...
Saved in:
| Main Authors: | , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2024-11-01
|
| Series: | Chemistry Proceedings |
| Subjects: | |
| Online Access: | https://www.mdpi.com/2673-4583/16/1/111 |
| Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
| Summary: | In this work, we synthesized methylxanthine and azobenzene derivatives, linked to secondary amines via a seven-carbon chain, to evaluate their acetylcholinesterase (AChE) inhibitory activity. Among the azobenzene compounds, <b>3a</b> exhibited the highest activity with an IC<sub>50</sub> of 1.1 µM. Meanwhile, the theobromine derivative <b>2a</b> was the most potent inhibitor among the methylxanthines, with an IC<sub>50</sub> of 0.19 µM. These results highlight the importance of structure–activity relationship analysis to optimize AChE inhibition by modifying pharmacophore fragments and secondary amines. |
|---|---|
| ISSN: | 2673-4583 |