1074-82-4Relevant academic research and scientific papers
Synthesis, Crystal Structure, Fluorescent and Antioxidation Properties of Cerium(III) and Europium(III) Complexes with Bis(3-methoxysalicylidene)-3-oxapentane-1,5-diamine
Tang, Xia,Shi, Xinkui,Xu, Yuling,Shen, Kesheng,Mao, Shanshan,Wu, Huilu
, p. 379 - 386 (2017)
Two aliphatic ether Schiff base lanthanide complexes (Ln = Eu, Ce) with bis(3-methoxysalicylidene)-3-oxapentane-1,5-diamine (Bod), were synthesized and characterized by physicochemical and spectroscopic methods. [Eu(Bod)(NO3)3] (1) is a discrete mononuclear species and [Ce(Bod)(NO3)3DMF]∞ (2) exhibits an inorganic coordination polymer. In the two complexes, the metal ions both are ten-coordinated and the geometric structure around the LnIII atom can be described as distorted hexadecahedron. Under excitation at room temperature, the red shift in the fluorescence band of the ligand in the complexes compared with that of the free ligand can be attributed to coordination of the rare earth ions to the ligand. Moreover, the antioxidant activities of the two complexes were investigated. The results demonstrated that the complexes have better scavenging activity than both the ligand and the usual antioxidants on the hydroxyl and superoxide radicals.
Enhancing insulin sensitivity by dual PPARγ partial agonist, β-catenin inhibitor: Design, synthesis of new αphthalimido-o-toluoyl2-aminothiazole hybrids
Mourad, Ahmed A. E.,Mourad, Mai A. E.
, (2020)
Aims: Partial PPARγ agonists attracted substantially heightened interest as safer thiazolidinediones alternatives. On the other hand, Wnt/β-catenin antagonists have been highlighted as promising strategy for type 2 diabetes management via up-regulating PPARγ gene expression. We aimed at synthesizing novel partial PPARγ agonists with β-catenin inhibitory activity which could enhance insulin sensitivity and avoid the side effects of full PPARγ agonists. Main methods: We synthesized novel series of α-phthlimido-o-toluoyl-2-aminothiazoles hybrids for evaluating their antidiabetic activity and discovering its mechanistic pathway. We assessed effect of the new hybrids on PPARγ activation using a luciferase reporter assay system. Moreover, intracellular triglyceride levels, gene levels of c/EBPα, PPARγ and PPARγ targets including GLUT4, adiponectin, aP2 were measured in 3T3-L1 cells. Uptake of 2-DOG together with PPARγ and β-catenin protein levels were evaluated in 3T3-L1cells. In addition, molecular docking studies with PPARγ LBD, physicochemical properties and structure activity relationship of the novel hybrids were also studied. Key findings: Three of the synthesized hybrids showed partial PPARγ agonistic activity and distinct PPARγ binding pattern. These compounds modulated PPARγ gene expression and PPARγ target genes; and increased glucose uptake in 3T3-L1 and slightly induced adipogenesis compared to rosiglitazone. Moreover, these compounds reduced β-catenin protein level which reflected in increased both PPARγ gene and protein levels that leads to improved insulin sensitivity and increased GLUT4 and adiponectin gene expression. Significance: Our synthesized compounds act as novel partial PPARγ agonists and β-catenin inhibitors that have potent insulin sensitizing activity and mitigate the lipogenic side effects of TZDs.
Synthesis and Characterization of Novel Phthalimide-pyrano[3,2-c]chromene and Phthalimide-pyrano-2-one Hybrids
Sameem, Bilqees,Saeedi, Mina,Mahdavi, Mohammad,Nadri, Hamid,Vafadarnejad, Fahimeh,Amini, Mohsen
, p. 1678 - 1684 (2018)
Coumarin skelton holds substantial promise for further exploration because of its immense pharmacological potential. In this pursuit, a series of phthalimide-chromen and phthalimide-pyran-2-one hybrids were synthesized in efficient yields via one-pot multicomponent reaction of aldehyde linked to phthalimide moiety, 4-hydroxy coumarin/4-hydroxy-6-methyl-2H-pyran-2-one, and malanonitrile by Knoevenagel reaction at room temperature in the presence of DABCO as catalyst. The compounds were characterized by 1H NMR and 13C NMR, MS, and FTIR. All the compounds consisting of phthalimide-chromen/pyrano-2-one moieties tethered by spacers of varying lengths were evaluated for their biological activity in Ellman's assay. Most of the compounds feebly inhibited Acetylcholinesterase Enzyme and were inactive toward Butyrylcholinesterase Enzyme.
A mesogenic triphenylene-perylene-triphenylene triad
Kong, Xiangfei,He, Zhiqun,Zhang, Yinning,Mu, Linping,Liang, Chunjun,Chen, Bo,Jing, Xiping,Cammidge, Andrew N.
, p. 764 - 767 (2011)
A straightforward synthesis of triphenylene-perylene-triphenylene triad structures has been achieved by using versatile triphenylene intermediates bearing a single oxyalkyl amine side chain. Among these, PBITP10 showed a stable columnar mesophase implying favorably matched core-core separations in the structure. Importantly, the triad can be used as a vehicle for doping columnar triphenylene matrices with functional but incompatible perylene units and a mixture of hexahexyloxytriphenylene matrix doped with 0.1% PBITP10 is homogeneous and liquid crystalline.
Redox-active binary eutectics: Preparation and their electrochemical properties
Chen, Hui,Niu, Zhihui,Zhao, Yu
, (2021)
Eutectics are emerging as promising candidate for electrochemical energy storage. However, the eutectics usually show high viscosity that usually arises from strong intermolecular interactions greatly limits their application. In this communication, we design and prepare two redox-active molecules that both are able to form binary eutectics with TBMA-TFSI. Combined experimental and computational studies indicate the intermolecular interaction is weakened after eutectic formation, resulting in decreased viscosity and enhanced ionization ratio of TBMA-TFSI without affecting the redox behaviors of the individual molecules. Further, the redox-active binary eutectic is used as solvent-free electrolyte for battery application.
Monofluorinated Nitrogen Containing Heterocycles: Synthesis, Characterization and Fluorine Effect
Reichel, Marco,Karaghiosoff, Konstantin
, p. 1790 - 1794 (2020)
A straight forward synthesis and efficient introduction of fluoromethyl group in nitrogen heterocycles is reported. Starting from the respective NH heterocycles fluoromethylation is performed with fluoroiodomethane and proceeds under mild reaction conditions. Structural information of monofluoromethylated nitrogen-containing cyclic compounds containing the biologically active NCH2F moiety are reported. The particularly impressively change of physical and spectroscopic properties by the substitution of a methyl group by a monofluoromethyl group is discussed based on these examples.
Design, synthesis and preliminary bioactivity evaluation of bitopic benzopyranomorpholine analogues as selective dopamine D3 receptor ligands as anti-drug addiction therapeutic agents
Cai, Jin,Chen, Xixi,Huang, Mingqi,Ji, Min,Wang, Yuhong
, (2021/08/09)
Three series of bitopic benzopyranomorpholine analogues were designed, synthesized, and evaluated as a novel class of selective ligands for the dopamine D3 receptor. Binding affinities of target compounds were determined using the method of radioligand binding assay. Most compounds demonstrated considerable binding affinities and selectivity for D3 receptor. Besides, the compounds were screened for their ability to alleviate withdrawal symptoms of opioid addiction in animal behavioral models. The results showed that compound 20h displayed nanomolar affinity for the D3R, and exhibited anti-drug addiction efficacy in the animal model of of naloxone-induced withdrawal symptoms in morphine-dependent mice.
SYNTHESIS OF 2-(2-AMINOETHOXY) ETHANOL
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Paragraph 0061-0062, (2021/02/12)
A method for synthesizing 2-(2-aminoethoxy) ethanol, including the steps of producing 2-(2-phthalimidoethoxy) ethanol by reacting 5-tosyloxy-3-oxapentanol with potassium phthalate and converting the 2-(2-phthalimidoethoxy) ethanol to the 2-(2-aminoethoxy) ethanol by reacting the 2-(2-phthalimidoethoxy) ethanol with hydrazine monohydrate. Reacting the 2-(2-phthalimidoethoxy) ethanol with the hydrazine monohydrate may include forming a final mixture by adding the hydrazine monohydrate to a solution of 2-(2-phthalimidoethoxy) ethanol, refluxing the final mixture in a nitrogen atmosphere, extracting a second organic phase containing the 2-(2-aminoethoxy) ethanol from the final mixture using a second portion of chloroform, and purifying the 2-(2-aminoethoxy) ethanol from the second organic phase.
Dinotefuran hapten, colloidal gold labeled dinotefuran monoclonal antibody and dinotefuran colloidal gold detection device (by machine translation)
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Paragraph 0029; 0033-0035; 0043, (2020/09/20)
The invention belongs to the technical field of biological detection, and particularly relates to a dinotefuran hapten and dinotefuran colloidal gold detection device and a preparation method thereof. Compared with the prior art, the dinotefuran colloidal gold detection device has the advantages of being convenient to use, economical, rapid, easy to manufacture and low in cost. (by machine translation)
BIOISPIRED PROTEASOME ACTIVATORS WITH ANTIAGEING ACTIVITY
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Page/Page column 7; 19, (2019/10/01)
The present invention relates to novel bio-inspired hybrid compounds of formula I which act as proteasome activators and exhibit anti-ageing activity, as well as methods for their synthesis. These hybrid compounds combine the structural features of hydroxytyrosol and the natural antioxidant vitamin E or its bioisosteres in one molecular scaffold. The compounds of formula I, which include structural proteasome activators (activation by stereochemical interaction), can be used in the production of anti-ageing products, such as cosmetic preparations. Additionally, they can be used in conditions and diseases where the proteasome is down-regulated, as well as proteasome-activation control compounds.
