Synthesis and Biological Evaluation of Thiophene Derivatives as Acetylcholinesterase Inhibitors

Molecules

Mohamed M. Ismail¹  Mona M. Kamel¹  Lamia W. Mohamed¹  Samar I. Faggal¹ 

[1] ¹Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, El-Kasr El-Aini Street, Cairo 11562, Egypt ²Pharmacology and Toxicology Department, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt

关键词: thiophene;    Gewald;    Ellman;    acetylcholinesterase;    Alzheimer’s disease;   

DOI  :  10.3390/molecules17067217

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.