Next Article in Journal
Astragalus membranaceus Extract Activates Immune Response in Macrophages via Heparanase
Previous Article in Journal
Liquiritigenin Inhibits Tumor Growth and Vascularization in a Mouse Model of Hela Cells
Molecules 2012, 17(6), 7217-7231; doi:10.3390/molecules17067217
Article

Synthesis and Biological Evaluation of Thiophene Derivatives as Acetylcholinesterase Inhibitors

1, 1, 1,* , 1 and 2
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 / Revised: 31 May 2012 / Accepted: 5 June 2012 / Published: 12 June 2012
(This article belongs to the Section Medicinal Chemistry)
Download PDF [380 KB, uploaded 18 June 2014]

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 thiophene; Gewald; Ellman; acetylcholinesterase; Alzheimer’s disease
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Share & Cite This Article

Export to BibTeX |
EndNote


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.

View more citation formats

Related Articles

Article Metrics

Comments

Citing Articles

[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert