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

Synthesis and Biological Evaluation of Thiophene Derivatives as Acetylcholinesterase Inhibitors

1, 1, 1,* email, 1 and 2
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)
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.
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
PDF Full-text Download PDF Full-Text [380 KB, uploaded 18 June 2014 19:49 CEST]

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.

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