Category: 6850-57-3

Xie, Hong-Xu published the artcileNovel tetrahydrobenzo[b](thiophen-2-yl)urea derivatives as novel α-glucosidase inhibitors: Synthesis, kinetics study, molecular docking, and in vivo anti-hyperglycemic evaluation, Application In Synthesis of 6850-57-3, the publication is Bioorganic Chemistry (2021), 105236, database is CAplus and MEDLINE.

α-Glucosidase inhibitors, which can inhibit the digestion of carbohydrates into glucose, are one of important groups of anti-type 2 diabetic drugs. In the present study, we report our effort on the discovery and optimization of α-glucosidase inhibitors with tetrahydrobenzo[b](thiophen-2-yl)urea core. Screening of an inhouse library revealed a moderated α-glucosidase inhibitors, 5a, and then the following structural optimization was performed to obtain more efficient derivatives Most of these derivatives showed increased inhibitory activity against α-glucosidase than the parental compound 5a (IC₅₀ of 26.71 ± 1.80 μM) and the pos. control acarbose (IC₅₀ of 258.53 ± 1.27 μM). Among them, compounds 8r (IC₅₀ = 0.59 ± 0.02 μM) and 8s (IC₅₀ = 0.65 ± 0.03 μM) were the most potent inhibitors, and showed selectivity over α-amylase. The direct binding of both compounds with α-glucosidase was confirmed by fluorescence quenching experiments Kinetics study revealed that these compounds were non-competitive inhibitors, which was consistent with the mol. docking results that compounds 8r and 8s showed high preference to bind to the allosteric site instead of the active site of α-glucosidase. In addition, compounds 8r and 8s were not toxic (IC₅₀ > 100 μM) towards LO2 and HepG2 cells. Finally, the in vivo anti-hyperglycemic activity assay results indicated that compounds 8r could significantly decrease the level of plasma glucose and improve glucose tolerance in SD rats treated with sucrose. The present study provided the (tetrahydrobenzo[b]thiophen-2-yl)urea chemotype for developing novel α-glucosidase inhibitors against type 2 diabetes.

Bioorganic Chemistry published new progress about 6850-57-3. 6850-57-3 belongs to ethers-buliding-blocks, auxiliary class Amine,Benzene,Ether, name is (2-Methoxyphenyl)methanamine, and the molecular formula is C9H6N2O2, Application In Synthesis of 6850-57-3.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Zhang, Xiaoying published the artcileNickel Complexes Bearing N,N,O-Tridentate Salicylaldiminato Ligand: Efficient Catalysts for Imines Formation via Dehydrogenative Coupling of Primary Alcohols with Amines, Product Details of C8H11NO, the publication is Organometallics (2021), 40(22), 3843-3853, database is CAplus.

Treatment of salicylaldiminato ligand L1H-L2H (L1H = 2,4-di-tert-butyl-6-((quinolin-8-ylimino)methyl)phenol; L2H = 2,4-di-tert-butyl-6-(((2-(diethylamino)ethyl)imino)methyl)phenol) with Ni(OAc)₂·4H₂O in refluxing EtOH afforded Ni complexes [(L1)Ni(OAc)] (1) and [(L2)Ni(OAc)] (2), resp. Reaction of L3H (L3H = (2,4-di-tert-butyl-6-(((2-(pyridin-2-yl)ethyl)imino)methyl)phenol)) with Ni(OAc)₂·4H₂O in the presence of excess triethylanmine gave the dual ligands coordinated Ni complex [(L2)₂Ni] (3). Complexes 1–3 were well characterized by high-resolution mass spectrometry, IR spectroscopy, elemental anal., and x-ray diffraction anal. All the three Ni(II) complexes exhibited efficient activity and good selectivity in the acceptorless dehydrogenative coupling of alcs. and amines to produce imines and diimines. The present protocol provides an atom-economical and sustainable route for the synthesis of various imine derivatives by employing an earth-abundant Ni salt and easily prepared salicylaldiminato ligands.

Organometallics published new progress about 6850-57-3. 6850-57-3 belongs to ethers-buliding-blocks, auxiliary class Amine,Benzene,Ether, name is (2-Methoxyphenyl)methanamine, and the molecular formula is C8H19NO2, Product Details of C8H11NO.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Wang, Shan published the artcileDesign, synthesis, and biological evaluation of 2,4-diamino pyrimidine derivatives as potent FAK inhibitors with anti-cancer and anti-angiogenesis activities, Category: ethers-buliding-blocks, the publication is European Journal of Medicinal Chemistry (2021), 113573, database is CAplus and MEDLINE.

A series of 2,4-diamino pyrimidine (DAPY) derivatives I (R¹ = 2-ClC₆H₄, 4-MeOC₆H₄, 4-BrC₆H₄, etc.), II (R² = 4-H₂NC₆H₄, 4-MeOC₆H₄, 2-O₂NC₆H₄, etc.) were designed, synthesized, and evaluated as inhibitors of focal adhesion kinase (FAK) with antitumor and anti-angiogenesis activities. Most compounds effectively suppressed the enzymic activities of FAK, and the IC₅₀s of I (R¹ = 2-ClC₆H₄) and II (R² = 2-MeOC₆H₄) were 2.75 and 1.87 nM, resp. They exhibited strong antiproliferative effects against seven human cancer cells, with IC₅₀ values against two FAK-overexpressing pancreatic cancer cells (PANC-1 and BxPC-3) of 0.98μM, 0.55μM, and 0.11μM, 0.15μM, resp. Moreover, the above two compounds obviously suppressed the colony formation, migration, and invasion of PANC-1 cells in a dose-dependent manner. Meanwhile, these two compounds could induce the apoptosis of PANC-1 cells and arrest the cell cycle in G2/M phase according to the flow cytometry assay. Western blot revealed that these compounds effectively inhibited the FAK/PI3K/Akt signal pathway and significantly decreased the expression of cyclin D1 and Bcl-2. In addition, the above compounds potently inhibited the antiproliferative of HUVECs and obviously altered the cell morphol and also significantly inhibited the migration, tube formation of HUVECs and severely impaired the angiogenesis in the zebrafish model. Overall, these results revealed the potential of these compounds as promising candidates for further preclin. studies.

European Journal of Medicinal Chemistry published new progress about 6850-57-3. 6850-57-3 belongs to ethers-buliding-blocks, auxiliary class Amine,Benzene,Ether, name is (2-Methoxyphenyl)methanamine, and the molecular formula is C10H9NO4S, Category: ethers-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

He, Ben published the artcileortho-Terphenylene Viologens with Through-Space Conjugation for Enhanced Photocatalytic Oxidative Coupling and Hydrogen Evolution, Application In Synthesis of 6850-57-3, the publication is Journal of the American Chemical Society (2022), 144(10), 4422-4430, database is CAplus and MEDLINE.

A series of novel ortho-terphenylene viologen derivatives (o-TPV²⁺) with through-space conjugation (TSC) via the combination of ortho-terphenylene skeletons with viologen structure is reported. Their optoelectronic properties can be adjusted by N-arylation or N-alkylation reactions. Compared with other viologen derivatives, o-TPV²⁺ not only exhibits strong photoluminescence, but also retards the charge recombination process and stabilizes diradicals state without forming a quinoid structure due to the special TSC effect. Based on their special redox characteristics, o-TPV²⁺ were applied to the photocatalytic oxidative coupling of benzylamine with 96% yield. In addition, pTA-o-TPV²⁺ (tethered with p-toluic acid) modified g-C₃N₄ was used for visible-light-driven hydrogen production for the first time, exceeding 15 times the rate over unmodified g-C₃N₄.

Journal of the American Chemical Society published new progress about 6850-57-3. 6850-57-3 belongs to ethers-buliding-blocks, auxiliary class Amine,Benzene,Ether, name is (2-Methoxyphenyl)methanamine, and the molecular formula is C8H11NO, Application In Synthesis of 6850-57-3.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Li, Zhibin published the artcileSelective electrochemical oxidation of aromatic hydrocarbons and preparation of mono/multi-carbonyl compounds, Quality Control of 6850-57-3, the publication is Science China: Chemistry (2021), 64(12), 2134-2141, database is CAplus.

A selective electrochem. oxidation was developed under mild condition. Various mono-carbonyl and multi-carbonyl compounds can be prepared from different aromatic hydrocarbons with moderate to excellent yield and selectivity by virtue of this electrochem. oxidation The produced carbonyl compounds can be further transformed into α-ketoamides, homoallylic alcs. and oximes in a one-pot reaction. In particular, a series of α-ketoamides were prepared in a one-pot continuous electrolysis. Mechanistic studies showed that 2,2,2-trifluoroethan-1-ol (TFE) can interact with catalyst species and generate the corresponding hydrogen-bonding complex to enhance the electrochem. oxidation performance.

Science China: Chemistry published new progress about 6850-57-3. 6850-57-3 belongs to ethers-buliding-blocks, auxiliary class Amine,Benzene,Ether, name is (2-Methoxyphenyl)methanamine, and the molecular formula is C8H11NO, Quality Control of 6850-57-3.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Xing, Chuanwang published the artcilePerylenetetracarboxylic diimide covalently bonded with mesoporous g-C₃N₄ to construct direct Z-scheme heterojunctions for efficient photocatalytic oxidative coupling of amines, Application In Synthesis of 6850-57-3, the publication is Applied Catalysis, B: Environmental (2021), 120534, database is CAplus.

Photocatalytic oxidative coupling of amines is a promising method for imine synthesis. In this paper, a robust covalently-bonded direct Z-scheme heterostructure (PDI/mpgCN) for photocatalytic oxidative coupling of amine was reported for the first time. Perylenetetracarboxylic diimide (PDI) mols. were covalently connected to the surface of mesoporous carbon nitride (mpgCN) via an in-situ condensation strategy. Compared with the poor conversion efficiency upon pristine g-C₃N₄, PDI/mpgCN heterostructure exhibits a remarkable enhancement on amine oxidation rate (AOR), with the optimal AOR reaches to as high as 20.63 mmol g^-1 h^-1 upon 20 % PDI/mpgCN. As far as we know, it is the highest AOR achieved so far for amine photooxidation coupling with heterojunction materials. Transient absorption studies proved the formation of Z-scheme junction, and efficient interfacial charge transfer. Our study not only makes an insight into the heterojunction design with chem. bond precision, but highlights the great prospects of Z-scheme photocatalyst in photo-chem. synthesis.

Applied Catalysis, B: Environmental published new progress about 6850-57-3. 6850-57-3 belongs to ethers-buliding-blocks, auxiliary class Amine,Benzene,Ether, name is (2-Methoxyphenyl)methanamine, and the molecular formula is C10H9IO4, Application In Synthesis of 6850-57-3.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Kang, Qiaoxiang published the artcileHollow multi-shelled In₂S₃ hierarchical nanotubes for enhanced photocatalytic oxidative coupling of benzylamine, Quality Control of 6850-57-3, the publication is Journal of Solid State Chemistry (2022), 123087, database is CAplus.

The unique structural features of the hollow and hierarchical structures give light to the developing categories of photocatalysts as a promising way to deal with the challenges involved in the process of heterogeneous photocatalysis. Herein, hollow multi-shelled In₂S₃ hierarchical nanotubes have been fabricated using NH₂-MIL-68 (In) as template and TAA. The results demonstrated that hollow multi-shelled In₂S₃ hierarchical nanotubes has been used as an efficient photocatalyst for the coupling of benzylamines under visible light irradiation and aerobic or anaerobic conditions, which burst out of the shackles of the reported reaction conditions. And the conversion and selectivity reached 74% and 99%, resp. The hierarchical structure with nanosheet on the surface of hollow multi-shelled nanotube have effectively promote the mass transfer and photogenerated carrier separation, increasing the number of reactive points. Then, it also has proved that the hole (h⁺), the nitrogen-centered radical cations as well as the carbon-centered radicals were most important in the reaction. This work provides a novel concept for further design of unique structural photocatalyst for boosting the catalytic activity.

Journal of Solid State Chemistry published new progress about 6850-57-3. 6850-57-3 belongs to ethers-buliding-blocks, auxiliary class Amine,Benzene,Ether, name is (2-Methoxyphenyl)methanamine, and the molecular formula is C8H11NO, Quality Control of 6850-57-3.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Li, Zhen published the artcileAn S-scheme α-Fe₂O₃/Cu₂O photocatalyst for an enhanced primary amine oxidative coupling reaction under visible light, Safety of (2-Methoxyphenyl)methanamine, the publication is Dalton Transactions (2022), 51(27), 10578-10586, database is CAplus and MEDLINE.

Here, an S-scheme α-Fe₂O₃/Cu₂O heterojunction photocatalyst was designed and fabricated for the primary amines oxidative coupling reaction to give aryl imines. On account of that, the S-scheme structure effectively separated the photogenerated electron-hole pairs and enhanced the photoredox ability of the photocatalytic system. The α-Fe₂O₃/Cu₂O composite could also enhance the reactivity to a large extent. This work will provide new insight into the design of photocatalysts with a more reasonable structure and higher performance.

Dalton Transactions published new progress about 6850-57-3. 6850-57-3 belongs to ethers-buliding-blocks, auxiliary class Amine,Benzene,Ether, name is (2-Methoxyphenyl)methanamine, and the molecular formula is C8H11NO, Safety of (2-Methoxyphenyl)methanamine.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Zhao, Lingyue published the artcileDesign, synthesis, and biological evaluation of arylmethylpiperidines as Kv1.5 potassium channel inhibitors, Product Details of C8H11NO, the publication is Journal of Enzyme Inhibition and Medicinal Chemistry (2022), 37(1), 462-471, database is CAplus and MEDLINE.

Kv1.5 potassium channel, encoded by KCNA5, is a promising target for the treatment of atrial fibrillation, one of the common arrhythmia. A new series of arylmethylpiperidines derivatives based on were synthesized and evaluated for their ability to inhibit Kv1.5 channel. Among them, compound showed good inhibitory activity (IC50 = 0.72 μM), preferable anti-arrhythmic effects and favored safety. These results indicate that can be a promising Kv1.5 inhibitor for further studies.

Journal of Enzyme Inhibition and Medicinal Chemistry published new progress about 6850-57-3. 6850-57-3 belongs to ethers-buliding-blocks, auxiliary class Amine,Benzene,Ether, name is (2-Methoxyphenyl)methanamine, and the molecular formula is C4H5NS2, Product Details of C8H11NO.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem

Zhang, Kaiyue published the artcileVisible-light-induced selective oxidation of amines into imines over UiO-66-NH₂@Au@COF core-shell photocatalysts, HPLC of Formula: 6850-57-3, the publication is ACS Sustainable Chemistry & Engineering (2021), 9(37), 12623-12633, database is CAplus.

Efficient and stable photocatalysts for selective oxidative coupling of amines to imines are crucial to the conversion of sustainable solar energy to value-added chem. energy. In this work, UiO-66-NH₂@Au@COF core-shell nanocomposites with intercalated Au nanoparticles between the UiO-66-NH₂ core and the covalent-organic framework (COF) shell have been demonstrated to exhibit enhanced activity and stability for visible-light-driven aerobic selective oxidation of amines to imines. With optimized Au and two-dimensional π-conjugated COF content, the obtained UiO-66-NH₂@Au_0.5@COF1 photocatalyst exhibited the highest conversion of benzylamine with an imine yield of 66.9% for at least five cycles. It is revealed that the introduction of appropriate Au and COF could not only broaden the visible-light absorption band but also promote the separation of photoinduced charge carriers and enhance the photocatalytic performance. Furthermore, a rational mechanism was explored to elucidate the process of photocatalytic reaction. The intercalated Au nanoparticles with the localized surface plasmon resonance (LSPR) effect act as generators of hot electrons and also transfer channels for the photo-generated electrons from the COF shell to the UiO-66-NH₂ core. Importantly, the MOF@metal@COF photocatalysts might provide a promising strategy to construct photocatalysts with desirable activity and stability under visible-light illumination.

ACS Sustainable Chemistry & Engineering published new progress about 6850-57-3. 6850-57-3 belongs to ethers-buliding-blocks, auxiliary class Amine,Benzene,Ether, name is (2-Methoxyphenyl)methanamine, and the molecular formula is C7H15NO, HPLC of Formula: 6850-57-3.

Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem