Molecules 2012, 17(6), 7217-7231; doi:10.3390/molecules17067217
Article

Synthesis and Biological Evaluation of Thiophene Derivatives as Acetylcholinesterase Inhibitors

1 Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, El-Kasr El-Aini Street, Cairo 11562, Egypt 2 Pharmacology and Toxicology Department, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt
* Author to whom correspondence should be addressed.
Received: 26 April 2012; in revised form: 31 May 2012 / Accepted: 5 June 2012 / Published: 12 June 2012
(This article belongs to the Section Medicinal Chemistry)
PDF Full-text Download PDF Full-Text [380 KB, uploaded 12 June 2012 12:14 CEST]
Abstract: A series of new thiophene derivatives has been synthesized using the Gewald protocol. The acetylcholinesterase inhibition activity was assayed according to Ellman’s method using donepezil as reference. Some of the compounds were found to be more potent inhibitors than the reference. 2-(2-(4-(4-Methoxyphenyl)piperazin-1-yl)acetamido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide (IIId) showed 60% inhibition, compared to only 40% inhibition by donepezil.
Keywords: thiophene; Gewald; Ellman; acetylcholinesterase; Alzheimer’s disease

Article Statistics

Load and display the download statistics.

Citations to this Article

Cite This Article

MDPI and ACS Style

Ismail, M.M.; Kamel, M.M.; Mohamed, L.W.; Faggal, S.I.; Galal, M.A. Synthesis and Biological Evaluation of Thiophene Derivatives as Acetylcholinesterase Inhibitors. Molecules 2012, 17, 7217-7231.

AMA Style

Ismail MM, Kamel MM, Mohamed LW, Faggal SI, Galal MA. Synthesis and Biological Evaluation of Thiophene Derivatives as Acetylcholinesterase Inhibitors. Molecules. 2012; 17(6):7217-7231.

Chicago/Turabian Style

Ismail, Mohamed M.; Kamel, Mona M.; Mohamed, Lamia W.; Faggal, Samar I.; Galal, Mai A. 2012. "Synthesis and Biological Evaluation of Thiophene Derivatives as Acetylcholinesterase Inhibitors." Molecules 17, no. 6: 7217-7231.

Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert