10215-07-3Relevant academic research and scientific papers
Design, synthesis and evaluation of 2-arylethenyl-N-methylquinolinium derivatives as effective multifunctional agents for Alzheimer's disease treatment
Xia, Chun-Li,Wang, Ning,Guo, Qian-Liang,Liu, Zhen-Quan,Wu, Jia-Qiang,Huang, Shi-Liang,Ou, Tian-Miao,Tan, Jia-Heng,Wang, Hong-Gen,Li, Ding,Huang, Zhi-Shu
, p. 139 - 153 (2017/03/02)
A series of 2-arylethenyl-N-methylquinolinium derivatives were designed and synthesized based on our previous research of 2-arylethenylquinoline analogues as multifunctional agents for the treatment of Alzheimer's disease (AD) (Eur. J. Med. Chem. 2015, 89, 349–361). The results of in vitro biological activity evaluation, including β-amyloid (Aβ) aggregation inhibition, cholinesterase inhibition, and antioxidant activity, showed that introduction of N-methyl in quinoline ring significantly improved the anti-AD potential of compounds. The optimal compound, compound a12, dramatically attenuated the cell death of glutamate-induced HT22 cells by preventing the generation of ROS and increasing the level of GSH. Most importantly, intragastric administration of a12?HAc was well tolerated at doses up to 2000 mg/kg and could traverse blood-brain barrier.
