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



Vafadarnejad F1 ; Saeedi M2, 3 ; Mahdavi M4 ; Rafinejad A1 ; Karimpourrazkenari E3 ; Sameem B5 ; Khanavi M6 ; Akbarzadeh T1, 3
Authors
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Authors Affiliations
  1. 1. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, P.O. Box: 14155-6451, Tehran, Iran
  2. 2. Medicinal Plants Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
  3. 3. Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, Iran
  4. 4. Endocrinology and Metabolism Research Center, Tehran University of Medical Sciences, Tehran, Iran
  5. 5. School of Pharmacy, International Campus (TUMS-IC), Tehran University of Medical Sciences, Tehran, Iran
  6. 6. Department of Pharmacognosy, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran

Source: Letters in Drug Design and Discovery Published:2017


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. © 2017 Bentham Science Publishers.
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