Title:Novel Indole-Isoxazole Hybrids: Synthesis and In Vitro Anti-Cholinesterase Activity
Volume: 14
Issue: 6
Author(s): Fahimeh Vafadarnejad, Mina Saeedi, Mohammad Mahdavi, Ali Rafinejad, Elahe Karimpour-Razkenari, Bilqees Sameem, Mahnaz Khanavi and Tahmineh Akbarzadeh*
Affiliation:
- Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences P.O. Box: 14155-6451, Tehran,Iran
Keywords:
Acetylcholinesterase, Alzheimer’s disease, Butyrylcholinesterase, Heterocycles, Indole, Isoxazole.
Abstract: Background: This work reports synthesis and in vitro cholinesterase inhibitory activity of
novel indole-isoxazole hybrids.
Method: The synthetic procedure was started from different ethyl 5-arylisoxazole-3-carboxylate
derivatives. Hydrolysis and reaction of the later compound with tryptamine afforded the desired
products in good yields.
Conclusion: Among the synthesized compounds, N-(2-(1H-indol-3-yl)ethyl)-5-(2-chlorophenyl)
isoxazole-3-carboxamide (4b) showed the best anti-cholinesterase activity.