Synthesis, docking study, and biological evaluation of novel umbellipherone/hymecromone derivatives as acetylcholinesterase/butyrylcholinesterase inhibitors
| Autor: | Hamid Nadri, Alireza Moradi, Farshad Homayouni Moghadam, Loghman Firoozpour, Bahar Pakseresht, Ali Ramazani, Alireza Foroumadi, Laleh Faraji, Setareh Moghimi, Zeinab Hasanpour, Mostafa Golshani, Mehdi Khoobi |
|---|---|
| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
Stereochemistry Organic Chemistry Triazole Substituent Acetylcholinesterase 03 medical and health sciences chemistry.chemical_compound 030104 developmental biology 0302 clinical medicine chemistry Docking (molecular) Moiety Amine gas treating General Pharmacology Toxicology and Pharmaceutics 030217 neurology & neurosurgery Butyrylcholinesterase Hymecromone |
| Zdroj: | Medicinal Chemistry Research. 27:1741-1747 |
| ISSN: | 1554-8120 1054-2523 |
| DOI: | 10.1007/s00044-018-2187-8 |
| Popis: | A novel hybrid series of umbellipherone and benzyl amine scaffolds, linked via triazole ring, was synthesized and evaluated as both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitors. Most of the synthesized compounds showed moderate to high activities by using Ellman’s modified assay. Among the target compounds, 6e bearing 3-methoxy substituent on benzyl moiety was the most active one (AChE and BuChE IC50 = 3.4 and 1.1 μM, respectively). Finally, binding modes of the target compound was studied using molecular docking stimulations. The neuroprotectivity evaluation exhibited that this compound efficiently protected PC12 neurons against H2O2-induced cell death. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full text from SpringerLink