Novel Multitarget-Directed Ligands Aiming at Symptoms and Causes of Alzheimer’s Disease was written by Wieckowska, Anna;Wichur, Tomasz;Godyn, Justyna;Bucki, Adam;Marcinkowska, Monika;Siwek, Agata;Wieckowski, Krzysztof;Zareba, Paula;Knez, Damijan;Gluch-Lutwin, Monika;Kazek, Grzegorz;Latacz, Gniewomir;Mika, Kamil;Kolaczkowski, Marcin;Korabecny, Jan;Soukup, Ondrej;Benkova, Marketa;Kiec-Kononowicz, Katarzyna;Gobec, Stanislav;Malawska, Barbara. And the article was included in ACS Chemical Neuroscience in 2018.Reference of 954-81-4 This article mentions the following:
Alzheimer’s disease (AD) is a major public health problem, which is due to its increasing prevalence and lack of effective therapy or diagnostics. The complexity of the AD pathomechanism requires complex treatment, e.g. multifunctional ligands targeting both the causes and symptoms of the disease. Here, we present new multitarget-directed ligands combining pharmacophore fragments that provide a blockade of serotonin 5-HT6 receptors, acetyl/butyrylcholinesterase inhibition, and amyloid β antiaggregation activity. Compound I has displayed balanced activity as an antagonist of 5-HT6 receptors (Ki = 18 nM) and noncompetitive inhibitor of cholinesterases (IC50hAChE = 14 nM, IC50eqBuChE = 22 nM). In further in vitro studies, compound I has shown amyloid β antiaggregation activity (IC50 = 1.27 μM) and ability to permeate through the blood-brain barrier. The presented findings may provide an excellent starting point for further studies and facilitate efforts to develop new effective anti-AD therapy. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Reference of 954-81-4).
N-(5-Bromopentyl)phthalimide (cas: 954-81-4) belongs to organobromine compounds. Many of the organo bromine compounds are relatively nonpolar. Bromine is more electronegative than carbon (2.8 vs 2.5) and hence the carbon in a carbonbromine bond is electrophilic in nature. When the molecular ion is detected, the bromine and chlorine isotope patterns are very distinct, but caution is to be exercised for certain mixed chlorinated/brominated compounds, which can look similar to homohalogen patterns.Reference of 954-81-4
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary