In 2022,Liu, Yulin; Uras, Giuseppe; Onuwaje, Itse; Li, Wenlong; Yao, Hong; Xu, Shengtao; Li, Xinuo; Li, Xinnan; Phillips, James; Allen, Stephanie; Gong, Qi; Zhang, Haiyan; Zhu, Zheying; Liu, Jie; Xu, Jinyi published an article in European Journal of Medicinal Chemistry. The title of the article was 《Novel inhibitors of AChE and Aβ aggregation with neuroprotective properties as lead compounds for the treatment of Alzheimer’s disease》.Recommanded Product: Ethyl 3-bromopropanoate The author mentioned the following in the article:
A series of sulfone analogs of donepezil I (R1 = H, F; R2 = H, 4-F, 3-Cl, etc.) were designed and synthesized as novel acetylcholinesterase (AChE) inhibitors with the potent inhibiting Aβ aggregation and providing neuroprotective effects as potential modalities for Alzheimer’s disease (AD). Most of the target compounds displayed effective inhibition of AChE, especially compound II which displayed powerful inhibitory activity (IC50 = 2.4 nM). Kinetic and docking studies indicated that compound II was a mixed-type inhibitor. Furthermore, in glyceraldehyde (GA)-exposed SH-SY5Y differentiated neuronal cells, compound II could potently inhibit AChE, reduce tau phosphorylation at S396 residue, provide neuroprotection by rescuing neuronal morphol. and increasing cell viability. It was also found to reduce amyloid aggregation in the presence of AChE. In addition, compound II showed evident protections from mitochondrial membrane dysfunction and oxidative stress in okadaic acid-induced pharmacol. models. Moreover, compound II exhibited more effective treatment prospects in vivo than donepezil, including a moderate blood-brain barrier permeability, a more potent AChE inhibitory activity and behavioral improvement in scopolamine-induced cognition-impaired mice model at a much lower dose. Collectively, compound II is a promising lead compound for further investigation to discovery and development of new anti-AD agents. The experimental process involved the reaction of Ethyl 3-bromopropanoate(cas: 539-74-2Recommanded Product: Ethyl 3-bromopropanoate)
Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact. Recommanded Product: Ethyl 3-bromopropanoate
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary