On February 1, 2017, Xiao, Ganyuan; Li, Yan; Qiang, Xiaoming; Xu, Rui; Zheng, Yunxiaozhu; Cao, Zhongcheng; Luo, Li; Yang, Xia; Sang, Zhipei; Su, Fu; Deng, Yong published an article.Quality Control of 4-Ethyl-piperazine-1-carbonyl chloride The title of the article was Design, synthesis and biological evaluation of 4′-aminochalcone-rivastigmine hybrids as multifunctional agents for the treatment of Alzheimer’s disease. And the article contained the following:
A series of 4′-aminochalcone-revastigmine hybrids were designed, synthesized and evaluated as multifunctional agents for the treatment of Alzheimer’s disease. The results showed that most of these compounds exhibited good multifunctional activities. In particular, compound 6c displayed the best inhibitory potency on acetylcholinesterase (IC50 = 4.91 μM), and significant antioxidative activity with a value 2.83-fold of Trolox. The kinetic anal. of AChE inhibition revealed that 6c showed mixed-type inhibition, binding simultaneously to the catalytic active site and peripheral anionic site of AChE. In addition, 6c inhibited self-induced Aβ1-42 aggregation and Cu2+-induced Aβ1-42 aggregation by 89.5% and 79.7% at 25 μM resp., as well as acted as a selective monoamine oxidase B inhibitor (IC50 = 0.29 μM) and a selective biometal chelator. Furthermore, 6c could cross the blood-brain barrier in vitro. Based on these results, Compound 6c could be considered as a very promising lead compound for Alzheimer’s disease. The experimental process involved the reaction of 4-Ethyl-piperazine-1-carbonyl chloride(cas: 53788-12-8).Quality Control of 4-Ethyl-piperazine-1-carbonyl chloride
The Article related to aminochalcone revastigmine hybrid synthesis blood brain barrier alzheimer disease, acetylcholinesterase inhibitors, alzheimer’s disease, aβ aggregation inhibitors, chalcone carbamate derivatives, monoamine oxidase b inhibitors, multifunctional agents and other aspects.Quality Control of 4-Ethyl-piperazine-1-carbonyl chloride
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics