NDLI: <i>N</i>-Aryl-substituted 3-(β-D-glucopyranosyloxy)-2-methyl-4(1<i>H</i>)-pyridinones as agents for Alzheimer's therapy

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Metallacycle-mediated cross-coupling with substituted and electronically unactivated alkenes

Morphology control for high performance organic thin film transistors

Coordination chemistry of group 13 monohalides

Switchable solvents

Gas-phase H/D-exchange reactions on resorcinarene and pyrogallarene capsules: Proton transport through a one-dimensional Grotthuss mechanism

DNA-templated combinatorial assembly of small molecule fragments amenable to selection/amplification cycles

Gold(i)-catalyzed intermolecular (4 + 2) cycloaddition of allenamides and acyclic dienes

Selective anion binding by a “Chameleon” capsule with a dynamically reconfigurable exterior

N-Aryl-substituted 3-(β-D-glucopyranosyloxy)-2-methyl-4(1H)-pyridinones as agents for Alzheimer's therapy

A synthesis of strychnine by a longest linear sequence of six steps

Tuning and optimizing the intrinsic interactions between phthalocyanine-based PPV oligomers and single-wall carbon nanotubes toward n-type/p-type

Prebiotically relevant mixed fatty acid vesicles support anionic solute encapsulation and photochemically catalyzed trans-membrane charge transport

Molecular anchors in the solid state: Restriction of intramolecular rotation boosts emission efficiency of luminogen aggregates to unity

A fully self-assembled non-symmetric triad for photoinduced charge separation

Synthesis of catalytically active porous organic polymers from metalloporphyrin building blocks

Proximity-driven metallopeptide catalysis: Remarkable side-chain scope enables modification of the Fos bZip domain

Solid-state dynamic combinatorial chemistry: reversibility and thermodynamic product selection in covalent mechanosynthesis

Metal-free and pH-controlled introduction of azides in proteins

Atomic-level control of the thermoelectric properties in polytypoid nanowires

Selective photocatalytic aerobic bromination with hydrogen bromide via an electron-transfer state of 9-mesityl-10-methylacridinium ion

Amino olefin nickel(i) and nickel(0) complexes as dehydrogenation catalysts for amine boranes

Luminescent cyclometalated platinum(ii) complexes containing N-heterocyclic carbene ligands with potent in vitro and in vivo anti-cancer properties accumulate in cytoplasmic structures of cancer cells

Passivating surface states on water splitting hematite photoanodes with alumina overlayers

Constitutionally selective amplification of multicomponent 84-membered macrocyclic hosts for (−)-cytidine•H⁺

A β-to-β 2,5-thienylene-bridged cyclic porphyrin tetramer: its rational synthesis and 1 : 2 binding mode with C₆₀

Controlling dynamic stereoisomerism in transition-metal folded baskets

Chemoselective enrichment for natural products discovery

A breakthrough method for the accurate addition of reagents in multi-step segmented flow processing

DNA-programmed spatial screening of carbohydrate–lectin interactions

Surface enhanced spatially offset Raman spectroscopic (SESORS) imaging – the next dimension

Molecular and electronic structure of cyclo[10]thiophene in various oxidation states: polaron pair vs. bipolaron

The modified-bead stretched sample method: Development and application to MALDI-MS imaging of protein localization in the spinal cord

Ultrasensitive water-processed monolayer photodetectors

Dehydration triggered asymmetric hydrogenation of 3-(α-hydroxyalkyl)indoles

Enantioselective silver-catalyzed propargylation of imines

Unique reactivity of Grignard reagents towards cyclopropenyl-carboxylates—highly selective carbon–carbon bond cleavage

A low-cost strategy for ⁴³Ca solid-state NMR spectroscopy

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Chemical Science Vol - 2 Issue - 3

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Chemical Science Vol -1

N-Aryl-substituted 3-(β-D-glucopyranosyloxy)-2-methyl-4(1H)-pyridinones as agents for Alzheimer's therapy

Content Provider	Royal Society of Chemistry (RSC)
Author	Lockman, Paul R. Patrick, Brian O. Allen, David D. Storr, Tim Scott, Lauren E. Rodríguez-Rodríguez, Cristina Telpoukhovskaia, Maria Orvig, Chris Thomas, Fancy Bowen, Meryn L. Green, David E. Merkel, Michael Page, Brent D. G. Adam, Michael J.
Copyright Year	2011
Abstract	Molecules designed to sequester, redistribute and/or remove metal ions are attractive therapeutic agents in neurodegenerative diseases such as Alzheimer's disease. The multifactorial nature of the condition and the generally poor target specificity associated with metal ion-binding therapy has led to the development of multifunctional 3-hydroxy-4-(1H)-pyridinone pro-ligands. The excellent qualities of the basic 3-hydroxy-4-pyridinone framework as a low toxicity metal chelator and an antioxidant, as well as its antibacterial and analgesic properties among other functions, inspired us to functionalize it with a framework derived from thioflavin-T, the well-known traditional dye used as a marker to detect amyloid deposits in tissue sections. Thus 2-methyl-3-hydroxy-1-(4-dimethylaminophenyl)-4(1H)-pyridinone (HL1), 2-methyl-3-hydroxy-1-(4-methylaminophenyl)-4(1H)-pyridinone (HL2), 1-(4-aminophenyl)-3-hydroxy-2-methyl-4(1H)-pyridinone (HL3), 1-(6-benzothiazolyl)-3-hydroxy-2-methyl-4(1H)-pyridinone (HL4), 1-(2-benzothiazolyl)-3-hydroxy-2-methyl-4(1H)-pyridinone (HL5) and 2-methyl-3-hydroxy-1-[4-(4-bromophenyl)-2-thiazolyl]-4(1H)-pyridinone (HL6) were obtained. Glycosylation, as well as incorporation of structures mimicking those of known amyloid imaging agents, may target drug action to the site of interest, the metal-overloaded amyloid plaques in the Alzheimer's brain. The pro-ligands were assessed for their antioxidant activity, cytotoxicity and ability to interfere with metal ion-induced amyloid peptide aggregation to screen promising lead compounds. Finally, in a brain uptake study with a radiolabeled glucoconjugate pyridinone, 3-(β-D-glucopyranosyloxy)-1-[4-(4-[125I]iodophenyl)-2-thiazolyl]-2-methyl-4(1H)-pyridinone ([125I]-GL7) was shown to cross the blood–brain barrier using an in situ rat brain perfusion technique.
Starting Page	642
Ending Page	648
Page Count	7
File Format	HTM / HTML PDF
ISSN	20416520
Volume Number	2
Issue Number	4
Journal	Chemical Science
DOI	10.1039/c0sc00544d
Language	English
Publisher	Royal Society of Chemistry
Access Restriction	Open
Subject Keyword	Hamble River H.L.1 Seaplane Dye Analgesic Iodine-125 Perfusion Chelation Cytotoxicity Blood\u2013brain barrier Glycosylation Amyloid Antioxidant Peptide
Content Type	Text
Resource Type	Article
Subject	Chemistry

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N-Aryl-substituted 3-(β-D-glucopyranosyloxy)-2-methyl-4(1H)-pyridinones as agents for Alzheimer's therapy

A copper–amyloid-β targeted fluorescent chelator as a potential theranostic agent for Alzheimer's disease

The ferromagnetic [Ln₂Co₆] heterometallic complexes

Efficient and selective separation of aqueous sulfate through recognition and precipitation

Proton and metal binding by cyclen-based highly rigid cryptands

Inhibition of beta-amyloid toxicity by short peptides containing N-methyl amino acids

Probing the magnetic relaxation and magnetic moment arrangement in a series of Dy₄ squares

Synthesis of novel heterobimetallic copper(i) hydrazone Schiff base complexes: A comparative study on the effect of heterocyclic hydrazides towards interaction with DNA/protein, free radical scavenging and cytotoxicity

Half-sandwich complexes of iridium and ruthenium containing cysteine-derived ligands

N-Aryl-substituted 3-(β-D-glucopyranosyloxy)-2-methyl-4(1H)-pyridinones as agents for Alzheimer's therapy

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