Application of 3395-91-3In 2020 ,《Tacrine-hydroxamate derivatives as multitarget-directed ligands for the treatment of Alzheimer’s disease: Design, synthesis, and biological evaluation》 was published in Bioorganic Chemistry. The article was written by Xu, Ana; He, Feng; Zhang, Xiangna; Li, Xiaoyang; Ran, Yingying; Wei, Chao; James Chou, C.; Zhang, Rui; Wu, Jingde. The article contains the following contents:
In order to develop multitarget-directed ligands as potential treatments for Alzheimer’s disease, twenty-eight new tacrine-hydroxamate derivatives were designed, synthesized, and biol. evaluated. As expected, most of the compounds exhibited inhibitory activities against cholinesterases (ChEs) and histone deacetylase (HDACs). Among the tested compounds, I showed not only potent and selective inhibition on AChE at sub-nanomolar potency (AChEIC50 = 0.12 nM, BChEIC50 = 361.52 nM) but also potent inhibition on HDAC (IC50 = 0.23 nM). Moreover, I exhibited inhibitory activity on Aβ1-42 self-aggregation as well as disaggregation activity on pre-formed Aβ fibrils. Furthermore, I exhibited antioxidant activity and metal chelating properties. Further mechanistic studies demonstrated that I is a pan-inhibitor of HDACs and a mixed-type inhibitor for AChE. It was shown that I is a BBB penetrant by online prediction. Taken together, the results indicate that I can serve as a lead compound to develop promising candidate analogs as AD therapeutics. In the experiment, the researchers used Methyl 3-bromopropanoate(cas: 3395-91-3Application of 3395-91-3)
Methyl 3-bromopropanoate(cas: 3395-91-3) belongs to bromides. One prominent application of synthetic organobromine compounds is the use of polybrominated diphenyl ethers as fire-retardants, and in fact fire-retardant manufacture is currently the major industrial use of the element bromine.Application of 3395-91-3
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary