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Novel Indole-Isoxazole Hybrids: Synthesis and In Vitro Anti-Cholinesterase Activity

[ Vol. 14 , Issue. 6 ]

Author(s):

Fahimeh Vafadarnejad, Mina Saeedi, Mohammad Mahdavi, Ali Rafinejad, Elahe Karimpour-Razkenari, Bilqees Sameem, Mahnaz Khanavi and Tahmineh Akbarzadeh   Pages 712 - 717 ( 6 )

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.

Keywords:

Acetylcholinesterase, Alzheimer’s disease, Butyrylcholinesterase, Heterocycles, Indole, Isoxazole.

Affiliation:

Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Medicinal Plants Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Research Institute, Tehran University of Medical Sciences, Tehran, Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, School of Pharmacy, International Campus (TUMS-IC), Tehran University of Medical Sciences, Tehran, Department of Pharmacognosy, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences P.O. Box: 14155-6451, Tehran

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