In 2019,Molecules included an article by Barre, Anais; Azzouz, Rabah; Gembus, Vincent; Papamicael, Cyril; Levacher, Vincent. Category: ethers-buliding-blocks. The article was titled 《Design, synthesis, and in-vitro biological activities of a bio-oxidizable prodrug to deliver both ChEs and DYRK1A inhibitors for AD therapy》. The information in the text is summarized as follows:
Despite their side effects, cholinesterase (ChE) inhibitors remain the only approved drugs to treat Alzheimer’s disease patients, along with the N-methyl-d-aspartate (NMDA) receptor antagonist memantine. In the last few years, the dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) has also been studied as a promising target for the development of new drugs for this pathol. In this context and based on previous characterization of bio-oxidizable prodrugs of potent acetylcholinesterase (AChE) inhibitors, a strategy involving the synthesis of a bio-oxidizable prodrug of both ChE and DYRK1A inhibitors was reported. To this end, a known potent inhibitor of DYRK1A, namely INDY was identified. The designed prodrug of both ChE and DYRK1A inhibitors was successfully synthesized, connecting both inhibitors by a carbonate link. This prodrug and its corresponding drug were then evaluated as ChEs and DYRK1A inhibitors. Remarkably, in-vitro results were in accordance with the starting hypothesis, showed a relative inactivity of the prodrug against DYRK1A and ChEs and a potent inhibition of ChEs by the oxidized form. Mol. docking and kinetic studies of ChE inhibition by the active compound were also discussed in this report. In the experiment, the researchers used many compounds, for example, tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6Category: ethers-buliding-blocks)
tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6) belongs to ethers.Although ethers resist hydrolysis, they are cleaved by hydrobromic acid and hydroiodic acid. Hydrogen chloride cleaves ethers only slowly. Category: ethers-buliding-blocks
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem