Potential Diagnostic Imaging of Alzheimer’s Disease with Copper-64 Complexes That Bind to Amyloid-β Plaques was written by McInnes, Lachlan E.;Noor, Asif;Kysenius, Kai;Cullinane, Carleen;Roselt, Peter;McLean, Catriona A.;Chiu, Francis C. K.;Powell, Andrew K.;Crouch, Peter J.;White, Jonathan M.;Donnelly, Paul S.. And the article was included in Inorganic Chemistry in 2019.Electric Literature of C9H9BO4 This article mentions the following:
Amyloid-β plaques, consisting of aggregated amyloid-β peptides, are one of the pathol. hallmarks of Alzheimer’s disease. Copper complexes formed using positron-emitting copper radionuclides that cross the blood-brain barrier and bind to specific mol. targets offer the possibility of noninvasive diagnostic imaging using positron emission tomog. New thiosemicarbazone-pyridylhydrazone based ligands that incorporate pyridyl-benzofuran functional groups designed to bind amyloid-β plaques have been synthesized. The ligands form stable complexes with copper(II) (Kd = 10-18 M) and can be radiolabeled with copper-64 at room temperature Subtle changes to the periphery of the ligand backbone alter the metabolic stability of the complexes in mouse and human liver microsomes, and influenced the ability of the complexes to cross the blood-brain barrier in mice. A lead complex was selected based on possessing the best metabolic stability and brain uptake in mice. Synthesis of this lead complex with isotopically enriched copper-65 allowed us to show that the complex bound to amyloid-β plaques present in post-mortem human brain tissue using laser ablation-inductively coupled plasma-mass spectrometry. This work provides insight into strategies to target metal complexes to amyloid-β plaques, and how small modifications to ligands can dramatically alter the metabolic stability of metal complexes as well as their ability to cross the blood-brain barrier. In the experiment, the researchers used many compounds, for example, (5-Methoxybenzofuran-2-yl)boronic acid (cas: 551001-79-7Electric Literature of C9H9BO4).
(5-Methoxybenzofuran-2-yl)boronic acid (cas: 551001-79-7) belongs to benzofurans derivatives. Benzofuran derivatives are one of the most important oxygen-containing heterocycles. Benzofurans have also made significant and distinctive contributions to biology. They exhibit several biological activities that range from antioxidant, antitubercular, antiplasmodial, insecticidal.Electric Literature of C9H9BO4
Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem