On April 4, 2021, Hofmann, Julian; Ginex, Tiziana; Espargaro, Alba; Scheiner, Matthias; Gunesch, Sandra; Arago, Marc; Stigloher, Christian; Sabate, Raimon; Luque, F. Javier; Decker, Michael published an article.Recommanded Product: 91-16-7 The title of the article was Azobioisosteres of Curcumin with Pronounced Activity against Amyloid Aggregation, Intracellular Oxidative Stress and Neuroinflammation. And the article contained the following:
Many (poly-)phenolic natural products, for example, curcumin and taxifolin, had been studied for their activity against specific hallmarks of neurodegeneration, such as amyloid-β 42 (Aβ42) aggregation and neuroinflammation. Due to their drawbacks, arising from poor pharmacokinetics, rapid metabolism and even instability in aqueous medium, the biol. activity of azobenzene compounds carrying a pharmacophoric catechol group I [R = H, Cl, NO2, MeO, EtO, Oi-Pr; R1 = OH, MeO], which had been designed as bioisoteres of curcumin had been examined Mol. simulations revealed the ability of these compounds to form a hydrophobic cluster with Aβ42, which adopts different folds, affecting the propensity to populate fibril-like conformations. Furthermore, the curcumin bioisosteres exceeded the parent compound in activity against Aβ42 aggregation inhibition, glutamate-induced intracellular oxidative stress in HT22 cells and neuroinflammation in microglial BV-2 cells. The most active compound prevented apoptosis of HT22 cells at a concentration of 2.5μM (83% cell survival), whereas curcumin only showed very low protection at 10μM (21% cell survival). The experimental process involved the reaction of 1,2-Dimethoxybenzene(cas: 91-16-7).Recommanded Product: 91-16-7
The Article related to azobioisostere curcumin diastereoselective preparation intracellular oxidative stress neuroinflammation, amyloid aggregation neurotoxicity neuroprotection docking azobioisostere curcumin diastereoselective preparation, amyloid beta, bioisosterism, natural products, neuroprotectivity, replica-exchange molecular dynamics and other aspects.Recommanded Product: 91-16-7
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Ether – Wikipedia,
Ether | (C2H5)2O – PubChem