| Title : Synthesis and molecular docking studies of 5-trifluoromethoxy-2-indolinones as cholinesterase dual inhibitors - Soylu-Eter_2024_Future.Med.Chem_16_623 |
| Author(s) : Soylu-Eter O , Ozsoy N , Karali N |
| Ref : Future Med Chem , 16 :623 , 2024 |
| Abstract : Background: In Alzheimer's disease, butyrylcholinesterase (BuChE) activity gradually increases, while acetylcholinesterase (AChE) activity decreases or remains unchanged. Dual inhibitors have important roles in regulation of synaptic acetylcholine levels and progression of Alzheimer's disease. Methods: 1-(Thiomorpholin-4-ylmethyl)/benzyl-5-trifluoromethoxy-2-indolinones (6-7) were synthesized. AChE and BuChE inhibitory effects were investigated with Ellman's method. Molecular docking studies were performed for analyzing the possible binding interactions at active sites. Results: Compound 6g was the strongest inhibitor against both AChE (K(i) = 0.35 microM) and BuChE (K(i) = 0.53 microM). It showed higher inhibitory effects than both donepezil and galantamine. Moreover, compound 7m had a higher inhibitory effect than galantamine and the effect was comparable to that of donepezil against both AChE (K(i) = 0.69 microM) and BuChE (K(i) = 0.95 microM). Conclusion: The benzyl substitution compared with 1-(thiomorpholin-4-ylmethyl) group significantly increased both AChE and BuChE inhibitory effects. |
| ESTHER : Soylu-Eter_2024_Future.Med.Chem_16_623 |
| PubMedSearch : Soylu-Eter_2024_Future.Med.Chem_16_623 |
| PubMedID: 38470247 |
Soylu-Eter O, Ozsoy N, Karali N (2024)
Synthesis and molecular docking studies of 5-trifluoromethoxy-2-indolinones as cholinesterase dual inhibitors
Future Med Chem
16 :623
Soylu-Eter O, Ozsoy N, Karali N (2024)
Future Med Chem
16 :623