1,4-Substituted 4-(1H)-pyridylene-hydrazone-type inhibitors of AChE, BuChE, and amyloid-β aggregation crossing the blood-brain barrier was written by Prinz, Michaela;Parlar, Sulunay;Bayraktar, Gulsah;Alptuzun, Vildan;Erciyas, Ercin;Fallarero, Adyary;Karlsson, Daniela;Vuorela, Pia;Burek, Malgorzata;Forster, Carola;Turunc, Ezgi;Armagan, Guliz;Yalcin, Ayfer;Schiller, Carola;Leuner, Kristina;Krug, Manuel;Sotriffer, Christoph A.;Holzgrabe, Ulrike. And the article was included in European Journal of Pharmaceutical Sciences in 2013.Recommanded Product: 954-81-4 This article mentions the following:
Given the fundamentally multifactorial character of Alzheimer’s disease (AD), addressing more than one target for disease modification or therapy is expected to be highly advantageous. Here, following the cholinergic hypothesis, we aimed to inhibit both acetyl- and butyrylcholinesterase (AChE and BuChE) in order to increase the concentration of acetylcholine in the synaptic cleft. In addition, the formation of the amyloid β fibrils should be inhibited and already preformed fibrils should be destroyed. Based on a recently identified AChE inhibitor with a 1,4-substituted 4-(1H)-pyridylene-hydrazone skeleton, a substance library has been generated and tested for inhibition of AChE, BuChE, and fibril formation. Blood-brain barrier mobility was ensured by a transwell assay. Whereas the p-nitrosubstituted compound 18C shows an anti-AChE activity in the nanomolar range of concentration (IC50 = 90 nM), the bisnaphthyl substituted compound 20L was found to be the best overall inhibitor of AChE/BuChE and enhances the fibril destruction. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Recommanded Product: 954-81-4).
N-(5-Bromopentyl)phthalimide (cas: 954-81-4) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. In the pharmaceutical industry organo bromine derivatives are used as sedatives, vasodilators, antiseptic agents, and anticancer agents.Recommanded Product: 954-81-4
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary