Synthesis of New Indole Derivatives Structurally Related to Donepezil and Their Biological Evaluation as Acetylcholinesterase Inhibitors

doi:10.3390/molecules17054811

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Molecules 2012, 17(5), 4811-4823; doi:10.3390/molecules17054811

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Synthesis of New Indole Derivatives Structurally Related to Donepezil and Their Biological Evaluation as Acetylcholinesterase Inhibitors

Mohamed M. Ismail, Mona M. Kamel, Lamia W. Mohamed* and Samar I. Faggal

Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt

* Author to whom correspondence should be addressed.

Received: 26 March 2012; in revised form: 16 April 2012 / Accepted: 17 April 2012 / Published: 25 April 2012

(This article belongs to the Section Medicinal Chemistry)

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Abstract: New series of indole derivatives analogous to donepezil, a well known anti-Alzheimer and acetylcholinesterase inhibitor drug, was synthesized. A full chemical characterization of the new compounds is provided. Biological evaluation of the new compounds as acetylcholinesterase inhibitors was performed. Most of the compounds were found to have potent acetylcholinesterase inhibitor activity compared to donepezil as standard. The compound 1-(2-(4-(2-fluorobenzyl) piperazin-1-yl)acetyl)indoline-2,3-dione (IIId) was found to be the most potent.

Keywords: indole; isatin; oxindole; acetylcholinesterase inhibitors; Alzheimer; donepezil

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Cite This Article

MDPI and ACS Style

Ismail, M.M.; Kamel, M.M.; Mohamed, L.W.; Faggal, S.I. Synthesis of New Indole Derivatives Structurally Related to Donepezil and Their Biological Evaluation as Acetylcholinesterase Inhibitors. Molecules 2012, 17, 4811-4823.

AMA Style

Ismail MM, Kamel MM, Mohamed LW, Faggal SI. Synthesis of New Indole Derivatives Structurally Related to Donepezil and Their Biological Evaluation as Acetylcholinesterase Inhibitors. Molecules. 2012; 17(5):4811-4823.

Chicago/Turabian Style

Ismail, Mohamed M.; Kamel, Mona M.; Mohamed, Lamia W.; Faggal, Samar I. 2012. "Synthesis of New Indole Derivatives Structurally Related to Donepezil and Their Biological Evaluation as Acetylcholinesterase Inhibitors." Molecules 17, no. 5: 4811-4823.

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