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Letters in Drug Design & Discovery

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ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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Research Article

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

Author(s): Fahimeh Vafadarnejad, Mina Saeedi, Mohammad Mahdavi, Ali Rafinejad, Elahe Karimpour-Razkenari, Bilqees Sameem, Mahnaz Khanavi and Tahmineh Akbarzadeh*

Volume 14, Issue 6, 2017

Page: [712 - 717] Pages: 6

DOI: 10.2174/1570180813666161018124726

Price: $65

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.

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