Category: 551001-79-7

Synthesis and evaluation of 2-pyridylbenzothiazole, 2-pyridylbenzoxazole and 2-pyridylbenzofuran derivatives as ¹¹C-PET imaging agents for β-amyloid plaques was written by Swahn, Britt-Marie;Wensbo, David;Sandell, Johan;Sohn, Daniel;Slivo, Can;Pyring, David;Malmstroem, Jonas;Arzel, Erwan;Vallin, Michaela;Bergh, Margareta;Jeppsson, Fredrik;Johnson, Allan E.;Jureus, Anders;Neelissen, Jan;Svensson, Samuel. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2010.Formula: C9H9BO4 This article mentions the following:

The syntheses and SAR of new series of β-amyloid binding agents are reported. The effort to optimize signal-to-background ratios for these ligands are described. Compounds I (X = S, O) and II displayed desirable lipophilicity and pharmacokinetic properties. Compounds I (X = S, O) were evaluated with in vitro autoradiog. studies and in vivo in APP/PS1 transgenic mice. It is shown that it was possible to increase the signal-to-background ratios compared to PIB 1, as demonstrated by compounds I (X = S, O). In the experiment, the researchers used many compounds, for example, (5-Methoxybenzofuran-2-yl)boronic acid (cas: 551001-79-7Formula: C9H9BO4).

(5-Methoxybenzofuran-2-yl)boronic acid (cas: 551001-79-7) belongs to benzofurans derivatives. Benzofurans are compounds with a planar structure having 10 pi electrons that include the lone pair on oxygen atom, which makes it more susceptible to electrophilic attack. In nature, benzofurans have occupied an important role among the plant phenols & several pharmacologically active compounds.Formula: C9H9BO4

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

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) (K_d = 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

Technetium-99m Labeled Pyridyl Benzofuran Derivatives as Single Photon Emission Computed Tomography Imaging Probes for β-Amyloid Plaques in Alzheimer’s Brains was written by Cheng, Yan;Ono, Masahiro;Kimura, Hiroyuki;Ueda, Masashi;Saji, Hideo. And the article was included in Journal of Medicinal Chemistry in 2012.Category: benzofurans This article mentions the following:

Three novel ^99mTc-labeled pyridyl benzofuran derivatives were tested as potential probes for imaging β-amyloid plaques using single photon emission computed tomog. (SPECT). The ^99mTc and corresponding rhenium complexes were synthesized with bis(aminoethanethiol) (BAT) as a chelating ligand. All Re complexes showed affinity for Aβ(1-42) aggregates (K_i = 13.6-149.6 nM). Biodistribution experiments in normal mice revealed that the ^99mTc-labeled derivatives displayed sufficient uptake in the brain (1.41-1.80% ID/g at 2 min postinjection). Notably, [^99mTc]BAT-Bp-2 showed a good initial uptake (1.80% ID/g at 2 min) and a reasonable washout from the brain (0.79% ID/g at 60 min). Ex vivo autoradiog. with [^99mTc]BAT-Bp-2 revealed substantial labeling of β-amyloid plaques in sections of brain tissue from Tg2576 transgenic mice but not in the age-matched controls. [^99mTc]BAT-Bp-2 may be a potential SPECT probe for imaging β-amyloid plaques in Alzheimer’s brains. In the experiment, the researchers used many compounds, for example, (5-Methoxybenzofuran-2-yl)boronic acid (cas: 551001-79-7Category: benzofurans).

(5-Methoxybenzofuran-2-yl)boronic acid (cas: 551001-79-7) belongs to benzofurans derivatives. Benzofuran is a core structural unit found in many naturally occurring compounds with multidirectional biological activities. Benzofurans are stable towards alkali and readily polymerize on treatment with sulfuric acid, due to which they are useful for the preparation of low cost chemically relatively inert resins.Category: benzofurans

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem