Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
Molecules. 2012 Jun 12;17(6):7217-31. doi: 10.3390/molecules17067217.
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.
使用 Gewald 协议合成了一系列新的噻吩衍生物。根据 Ellman 法，使用多奈哌齐作为参考，测定乙酰胆碱酯酶抑制活性。一些化合物被发现比参考物具有更强的抑制作用。2-(2-(4-(4-甲氧基苯基)哌嗪-1-基)乙酰胺基)-4,5,6,7-四氢苯并[b]噻吩-3-甲酰胺（IIId）显示出 60%的抑制率，而多奈哌齐仅显示出 40%的抑制率。
