Synthesis, biological evaluation, and molecular docking study of novel 1,2,4-substituted triazoles as inhibitors of alzheimer’s disease
In order to explore effective acetyl and butyrylcholinesterase enzyme inhibitors, a library of fifteen synthetic 1,2,4-substituted triazoles (5–19) was established and characterized using IR and NMR spectroscopic techniques. Compounds 9 and 16 were found to be the most potent AChE (IC50 = 38.91 ± 0....
| الحاوية / القاعدة: | Journal of the Iranian Chemical Society |
|---|---|
| المؤلف الرئيسي: | |
| التنسيق: | مقال |
| اللغة: | English |
| منشور في: |
Springer Science and Business Media Deutschland GmbH
2022
|
| الوصول للمادة أونلاين: | https://www.scopus.com/inward/record.uri?eid=2-s2.0-85136203736&doi=10.1007%2fs13738-022-02617-5&partnerID=40&md5=589609b1bc9159007cbde7e5a83479d0 |
| الملخص: | In order to explore effective acetyl and butyrylcholinesterase enzyme inhibitors, a library of fifteen synthetic 1,2,4-substituted triazoles (5–19) was established and characterized using IR and NMR spectroscopic techniques. Compounds 9 and 16 were found to be the most potent AChE (IC50 = 38.91 ± 0.52 µM) and BChE (IC50 = 42.74 ± 0.42 µM) inhibitors, against the standard eserine (IC50 = 39.19 ± 0.05 µM for AChE and 46.62 ± 0.08 µM for BChE). In addition, binding interactions of potent inhibitors of AChE and BChE were studied using molecular docking. Compounds 9 and 16 were identified as promising dual inhibitors for AChE and BChE that may further be investigated to serve as lead molecules against Alzheimer’s disease. © 2022, Iranian Chemical Society. |
|---|---|
| تدمد: | 1735207X |
| DOI: | 10.1007/s13738-022-02617-5 |