Purity | Size | Price | VIP Price | USA Stock *0-1 Day | Global Stock *5-7 Days | Quantity | ||||||
{[ item.p_purity ]} | {[ item.pr_size ]} | Inquiry |
{[ getRatePrice(item.pr_usd, 1,1,item.pr_is_large_size_no_price) ]} {[ getRatePrice(item.pr_usd,item.pr_rate,1,item.pr_is_large_size_no_price) ]} |
{[ getRatePrice(item.pr_usd, 1,1,item.pr_is_large_size_no_price) ]} | Inquiry {[ getRatePrice(item.pr_usd,item.pr_rate,item.mem_rate,item.pr_is_large_size_no_price) ]} {[ getRatePrice(item.pr_usd,1,item.mem_rate,item.pr_is_large_size_no_price) ]} | {[ item.pr_usastock ]} | in stock Inquiry - | {[ item.pr_chinastock ]} | {[ item.pr_remark ]} in stock Inquiry - | Login | Inquiry |
Please Login or Create an Account to: See VIP prices and availability
Ru(ii)–arene azole complexes as anti-amyloid-β agents
Ryan M. Hacker ; Daniela M. Grimard ; Katie A. Morgan , et al. Dalton Trans.,2024,53,18845-18855. DOI: 10.1039/D4DT01740D PubMed ID: 39093049
More
Abstract: With the recent clinical success of anti-amyloid-β (Aβ) monoclonal antibodies, there is a renewed interest in agents which target the Aβ peptide of Alzheimer's disease (AD). Metal complexes are particularly well-suited for this development, given their structural versatility and ability to form stabile interactions with soluble Aβ. In this report, a small series of ruthenium–arene complexes were evaluated for their respective ability to modulate both the aggregation and cytotoxicity of Aβ. First, the stability of the complexes was evaluated in a variety of aqueous media where the complexes demonstrated exceptional stability. Next, the ability to coordinate and modulate the Aβ peptide was evaluated using several spectroscopic methods, including thioflavin T (ThT) fluorescence, dynamic light scattering (DLS), and transmission electron microscopy (TEM). Overall, the complex RuBO consistently gave the greatest inhibitory action towards Aβ aggregation, which correlated with its ability to coordinate to Aβ in solution. Furthermore, RuBO also had the lowest affinity for serum albumin, which is a key consideration for a neurotherapeutic, as this protein does not cross the blood brain barrier. Lastly, RuBO also displayed promising neuroprotective properties, as it had the greatest inhibition of Aβ-inducted cytotoxicity.
CAS No. : | 136-95-8 | MDL No. : | MFCD00005785 |
Formula : | C7H6N2S | Boiling Point : | - |
Linear Structure Formula : | (C7H4NS)NH2 | InChI Key : | UHGULLIUJBCTEF-UHFFFAOYSA-N |
M.W : | 150.20 | Pubchem ID : | 8706 |
Synonyms : |
|
Signal Word: | Warning | Class: | N/A |
Precautionary Statements: | P305+P351+P338 | UN#: | N/A |
Hazard Statements: | H302-H319 | Packing Group: | N/A |
GHS Pictogram: |
* All experimental methods are cited from the reference, please refer to the original source for details. We do not guarantee the accuracy of the content in the reference.
Yield | Reaction Conditions | Operation in experiment |
---|---|---|
General procedure: we started with the4-methyl-1-piperazine carbonyl chloride (Scheme 1). By reactionof this compound with the corresponding amine in dry pyridineas solvent, at room temperature, the urea derivative crystallizedas hydrochloride. The hydrochloride was dissolved in water, basifiedwith aqueous Na2CO3 (10%) and extracted with CH2Cl2. The organiclayer was dried over Na2SO4 and the solvent was removed toafford a residue, which was purified by chromatography column toobtain the corresponding ureas 1-5. |
Yield | Reaction Conditions | Operation in experiment |
---|---|---|
72% | In toluene; at 100℃; for 0.166667h;Microwave irradiation; Sealed tube; | General procedure: General Procedure (GP): In a MW sealed-tube equipped with a magnetic stirring bar, to a 0.5 M solution of aldehyde (1.0 equiv.) in anhydrous toluene [0.5 M], amine (1.0 equiv.) and isocyanide (1.0 equiv.) were added sequentially and the reaction mixture was MW-heated (100 oC,150 W) for 10 minutes. Then, the solvent was removed until dryness and the crude was immediately purified by silica-gel column chromatography using a mixture of hexanes with ethyl acetate (7/3; v/v) to afford the corresponding products 1a-w. |