JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
·
2019
·
IF 4.027
Yu-Heng Hu,Jie Yang,Yun Zhang,Ke-Chun Liu,Teng Liu,Jie Sun,Xiao-Jing Wang
The work is focused on the design of drugs that prevent and treat Alzheimer’s disease (AD) and its complications. A series of 3–(4-aminophenyl)-coumarin derivatives designed, synthesised, fully characterised and evaluated in vitro/vivo. The biological assay experiments showed that some compounds displayed a clearly selective inhibition for acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Among all compounds, compound 4m exhibited the highest AChE inhibition with an IC50 value of 0.091 ± 0.011 µM and compound 4k exhibited the highest BuChE inhibition with an IC50 value of 0.559 ± 0.017 µM. A zebrafish behaviour analyser (Zebrobox) was used to determine the behavioural effects of the active compound on the movement distance of the aluminium chloride-induced zebrafish. Compound 4m offered a potential drug design concept for the development of therapeutic or preventive agents for AD and its complications.
研究领域:
药理学
·
神经科学
·
药物设计
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高影响因子
International Journal of Electrochemical Science
·
2023
·
IF 1.5
Hui Sun,Baoyang Lu,Xuemin Duan,Jingkun Xu,Liqi Dong,Xiaofei Zhu,Kaixin Zhang,Dufen Hu,Shouli Ming
The copolymerization of 2’-aminomethyl-3, 4-ethylenedioxythiophene (EDOT-MeNH 2 ) and 3, 4-ethylenedioxythiophene (EDOT) was successfully performed electrochemically in acetonitrile (CH 3 CN) containing tetrabutylammonium hexafluorophosphate (Bu 4 NPF 6 ) as the supporting electrolyte by direct anodic oxidation of the monomer mixtures. A series of experiments with different monomer feed ratios were carried out to investigate the influence of monomer feed ratio on the electrochemical copolymerization and the overall properties of the copolymer films. As-formed novel copolymers owned both the advantages of poly(2’-aminomethyl-3, 4-ethylenedioxythiophene) (PEDOT-MeNH 2 ) and poly(3, 4-ethylenedioxythiophene) (PEDOT), i.e ., good electrochemical behavior, excellent electrochemical stability, and good thermal stability. Spectroelectrochemistry analysis of copolymer with the feed ratio of 1:1 reflected λ max due to the π–π* transition and polaron band formation was found to be 620 nm and the band gap ( E g ) was calculated as 1.67 eV. The structure, thermogravimetry and morphology of the copolymers were investigated by infrared spectroscopy, thermal analysis, and scanning electron microscopy, respectively.
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NEW JOURNAL OF CHEMISTRY
·
2022
·Vol. 47
·期 3
·1256-1267
·
IF 3.925
Lei Yin,Hui Yang Li,Tingting Ge,Yuchao Li,Cuncun Zuo,Ming Wang,GuangJun Cui,Haofei Huang,Lin Guo
A series of acid–base-loaded γ-Al2O3 catalysts was applied as the catalysts for the isomerization of 3/4-methyl-tetrahydro phthalic anhydride. With a basic metal (K or Na) as the basic source and phosphorus (P) as the acid source, γ-Al2O3 was modified by equal volume immersion. NH3/CO2-TPD, XRD, TEM/EDS, BET, and TGA were used to analyze the catalysts, and 15%-K/Al2O3 and 10%-P/Al2O3 were determined as the most appropriate catalysts. The isomers were qualitatively and quantitatively analyzed using nuclear magnetic resonance (1H-NMR) and infrared spectroscopy (IR), and the reaction mechanism for the isomer formation was proposed. With 3-MTHPA as the substrate, the acid/base reaction temperature was 165/150 °C, the reaction time was 3 h and the amount of the catalyst added was 3%. A new type of continuous isomeric fixed-bed reactor was designed. The stability of the catalyst was tested, and the activity loss was 4.6–6.6% after 10 hours of operation.
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JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
·
2024
·
IF 3.1
Baoyan Ding,Wei Meng,Xiaoling Zang,Zhihua Lv
A small molecule, (S)-ethyl 1-(3-(4-chlorophenoxy)-2-hydroxypropyl)-3-(4-methoxyphenyl)-1H-pyrazole-5-carboxylate (SEC), has been reported to be capable of suppressing metastasis of prostate cancer (PCa) cells. In this study, SEC was used to study the metabolic responses of PCa cell lines (LNCaP, PC3, and DU145) with different metastatic potential and the alterations of mTOR, p-mTOR, AMPK, and p-AMPK levels, when the PCa cells were inhibited. The ultra-high performance liquid chromatography-high resolution mass spectrometry (UHPLC-HRMS)-based analysis showed that SEC induced the decreases of intracellular metabolites including glutamic acid, glutamine, and histidine (LNCaP); creatinine, citric acid/isocitric acid, and aspartic acid (PC3); and spermidine, S-hydroxymethylglutathione, LPE (20:3), and palmitic amide (DU145), and the increases of intracellular LPC (18:0) (LNCaP); tyrosine, pyroglutamic acid/pyrroline hydroxycarboxylic acid (PC3); and tyrosine, phenylalanine, phenylacetylglycine, spermine, histidine, and choline (DU145). SEC also caused the decrease of extracellular N1-acetylspermidine (LNCaP), erythronic acid/threonic acid (PC3 and DU145), and nicotinic acid/picolinic acid (DU145), and the increase of extracellular 5’-methylthioadenosine (DU145). High metastatic PC3 and DU145 cells exhibited changes in aromatic amino acid metabolism including tyrosine metabolism, phenylalanine, tyrosine, and tryptophan metabolism, and phenylalanine metabolism (PC3 and DU145), TCA cycle (PC3), arginine and proline metabolism, and glycerophospholipid metabolism (DU145), different from the low metastatic LNCaP cells, which had changes in alanine, aspartate, and glutamate metabolism, and arginine biosynthesis. In addition, the levels of p-mTOR and p-AMPK were shown to be obviously downregulated and upregulated, respectively, in high metastatic PC3 and DU145 cells upon SEC inhibition, while this behavior was not detected in LNCaP cells.
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高影响因子
SYNTHETIC METALS
·
2024
·
IF 4
Hailan Zeng,Ruomei Wu,Yanan Li,Haiyun Jiang,Xiang Wang,Weili Zhang,Ziyu Li,Jun Zhang,Zhengrong Yan
In this work, the copolymers were successfully synthesized by electrochemical polymerization of two monomers, bithiophene (BT) and 3,4-ethylenedioxythiophene (EDOT), in a lithium perchlorate/propylene carbonate (LiClO 4 /PC) solution. The as-prepared were characterized with the aid of cyclic voltammetry, colorimetric analysis, Fourier transform infrared spectroscopy, and Ultraviolet-visible spectroscopy. The electrochromic and colorimetric properties of copolymers poly(2,2′-bithiophene-co-3,4-ethylenedioxythiophene) (P(BT-co-EDOT)) and homopolymer poly(2,2′-bithiophene) (PBT) in 0.1 M LiClO 4 /PC solution were investigated, and the coloring process based on the redox reaction of the film was observed. When an anodic potential is applied, the copolymer P(BT-co-EDOT) films show a color change from blue-purple to blue-gray changes, and the homopolymer PBT shows a color change from orange to brown. In addition, spectroelectrochemistry studies indicate that copolymer P(BT-co-EDOT) has a lower optical band gap (1.73–1.87 eV) than homopolymer PBT. The copolymers P(BT-co-EDOT) show a high optical contrast (36.65–42.62%) and coloration efficiency (215.8–296.6 cm 2 C −1 ). The copolymer P(BT1-co-EDOT1) demonstrates excellent redox cycling stability, with 90% of the original optical contrast maintained after 500 cycles, making it an ideal candidate for copolymers.
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JOURNAL OF APPLIED POLYMER SCIENCE
·
2011
·Vol. 124
·期 1
·109-115
·
IF 1.24
Jikui Wang,Guofeng Cai,Xudong Zhu,Xiaping Zhou
The oxidative chemical polymerization of 3, 4-ethylenedioxythiophene (EDOT) was conducted at room temperature in the presence of poly(styrene sulfonate) (PSS) as the doping agent, sodium supersulphate (Na 2 S 2 O 8 ) and ferric sulphate(Fe 2 (SO 4 ) 3 ) as the compound oxidant and deionized water as the solvent. In order to remove sodium ion (Na + ), ferric ion (Fe 3+ ), and sulfate ion (SO4 2− ), certain amount of ion exchanger was added after 24 h, the dark blue poly(3, 4-ethylenedioxythiophene) (PEDT)/PSS solution was obtained. The influence of different proportions of EDOT and PSS, different proportions of EDOT and the compound oxidant, different stirring rates on the morphology, and surface resistivity were discussed. The influence of pH value of the PEDT/PSS solution, the coating thickness, and soak time on the surface resistivity was investigated. Recipe and experimental conditions were optimized and the PEDT/PSS solution was obtained with excellent performance which has relatively low in surface resistance, good water tolerance, and light transmittance. © 2011 Wiley Periodicals, Inc. J Appl Polym Sci, 2012
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JOURNAL OF COLLOID AND INTERFACE SCIENCE
·
2019
·
IF 6.361
Jiadong Liu,Yijia Wang,Lei Wang
A polyvinylidene fluoride (PVDF) organic conductive membrane with photoelectric activity was successfully developed via printing of oxidant (FeCl 3 ·6H 2 O) layer by layer and then chemical vapor deposition (CVD) of Poly (3, 4-ethylenedioxythiophene) (PEDOT). Four kinds of membranes were prepared by changing the number of oxidant coatings layers. The structure and photoelectric properties of four membranes were well characterized. The photocurrent density of 3.7 × 10 −4 A indicated that the four-oxidant coating layers membrane achieved the best performance in photo-electricity activity. A comprehensive study of degradation efficiency under different photoelectric conditions was carried out. Results showed that the photoelectrocatalytic removal of tetracycline hydrochloride was 1.6 and 7.9 times higher than that of photocatalysis and photolysis, respectively, under a voltage of 3 V assisted with visible light irradiation. The anti-interference and stability tests in continuous filtration process demonstrated that the dissolved organic matters (DOMs) can result in a 30% fluctuation on removal rate. The streaming potential tests of DOMs adsorption on membrane surface indicated that the more obvious the adsorption phenomenon was, the degradation of tetracycline hydrochloride was weaker. The degradation intermediates were identified and pathways were proposed in this work. The photoelectrocatalysis of PEDOT modified PVDF membrane provided a new potential for water purification .
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JOURNAL OF ELECTRONIC MATERIALS
·
2019
·Vol. 48
·期 11
·7068-7075
·
IF 1.676
Li Shuhui,Zhou Ying,Cui Lijun,Ge Zhenhua,Feng Jing
In 2 O 3 (ZnO) k superlattice ceramics are promising oxide thermoelectric materials, as superlattice interfaces are effective in scattering phonons and filtering low-energy electrons to decrease thermal conductivity and improve the figure of merit ( ZT ) value. In this work, homologous compounds were prepared by solid-state reaction method using ZnO and In 2 O 3 as raw materials. Phase purity and crystal structure were characterized by x-ray diffraction, revealing that In 2 O 3 (ZnO) k crystallizes in an R3 m space group for odd k values and P6 3 /mmc for even k values. The study of thermoelectric (TE) properties showed that as k increased, the thickness of InO(ZnO)
+ 3
also increased, while the electrical conductivity, thermal conductivity, Seebeck coefficient, power factor and ZT value were all decreased. In 2 O 3 (ZnO) 3 samples obtained a maximum power factor of 651 μ W m −1 K −2 at 973 K, and also achieved a maximum ZT value of 0.24 at 973 K.
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Chinese Journal of Natural Medicines
·
2014
·
IF 0
De-Biao YAN,Dong-Ping ZHANG,Ming LI,Wen-Yuan LIU,Feng FENG,Bin DI,Qing-Long GUO,Ning XIE
To synthesize a series of 3-, 4-, and/or 11-trihydroxy modified bergenin derivatives and evaluated their cytotoxic activity in vitro . The phenolic hydroxyl groups of bergenin were protected by benzyl groups with benzyl bromide. Treatment of dibenzyl bergenin with the corresponding acid in the presence of EDC·HCl and DMAP in CH 2 Cl 2 , followed by hydrogenation over Pd/C catalysts, afforded derivatives of bergenin esters. All of the target compounds were identified by IR, MS, and 1 H NMR. Twenty-six novel and three known derivatives of bergenin esters were synthesized. Their cytotoxicity values were evaluated by the MTT assay on the inhibition of DU-145 and BGC-823 cells in vitro . Several triply-substituted ( 3a, 4a, 5a, 6a, 7a ) and doubly-substituted ( 8b, 9b ) bergenin derivatives exhibited higher cytotoxic activity than bergenin. The result showed that the size of substituents and the lipophilicity of the bergenin esters displayed an important role on their cytotoxic activity.
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KEY ENGINEERING MATERIALS
·
2013
·
IF 0
Yun Xia Jiang,Hu Jin Zuo,Yong Jia Shen,Feng Ping Yi
The Friedel-Crafts acylation reaction between 5-cyanoindole and 4-chlorobutyryl chloride was conducted in ionic liquid 1-buty-3-methylimidazolium chloroaluminate ([bmiCl/AlCl3), the major product was 5-cyano-3-(4-chlorobuty) indole. The structure of the product was characterized by Mass and 1H NMR spectra. When the molar ratio of AlCl3 to [bmiCl in [bmiCl/AlCl3 is at 1:1 or less, no 5-cyano-3-(4-chlorobuty) indole could be obtained. The suitable molar ratios of AlCl3 to [bmiCl in [bmiCl/AlCl3 were from 2:1 to 3:1, the yields of the major product were from 68% to 70%, respectively. When the molar ratio of [bmiCl/AlCl3 to 5-cyanoindole was less than 2:1, the acylation reaction was difficult to carry out, because 5-cyanoindole would be not totally dissolve in [bmiCl/AlCl3 under the situation.
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RUSSIAN JOURNAL OF GENERAL CHEMISTRY
·
2026
·Vol. 95
·期 12
·3886-3902
·
IF 0.8
Lv Yingmei,Shi Lele,Luo Xi,Huang Yuhang,Du Zhenting
Thiazolidine-2,4-dione (TZD), a privileged scaffold, is a versatile pharmacophore and outstanding sulphur-containing heterocyclic compound found in various drugs. In this work, forty-two substituted 5-arylidene-1,3-thiazolidine-2,4-diones derivatives have been designed and synthesized by introducing sulfonyl groups, benzoyl groups, and amide groups into 5-(3/4-hydroxybenzylidene)thiazolidine-2,4-dione through Knoevenagel condensation, and their antibacterial activities were evaluated in vitro. As a result, thirty-five compounds were new compounds, and seven compounds were known compounds. The in vitro assay results disclosed that compared with B/C-series, A-series compounds presented remarkable antimicrobial activity against S. aureus, E. faecalis , and E. faecium . All twenty-one synthesized A-series compounds exhibited excellent antibacterial activity against S. aureus (MIC 80 ≤ 128 µg/mL). Among these, three compounds demonstrated the highest anti- E. faecalis activities (MIC 80 = 8 µg/mL), while E. faecium showed antibacterial susceptibility to A-series compounds except two of the investigated compounds p -cyanophenyl and p -trifluoromethoxyphenyl substituted sulfonate esters. In contrast, the B-series displayed limited activity, with only three compounds showing measurable anti- S. aureus effects, among which substituted phenyl benzoates exhibited the best antibacterial action against E. faecium (MIC 80 = 64 µg/mL). The C-series compounds demonstrated the weakest activity profile, with two N -substituted acetamides ( N -phenyl and N -methylphenyl) displaying moderate anti- S. aureus activity (MIC 80 = 128 µg/mL), which merely compound N - o -nitrophenyl was sensitive to E. faecalis (MIC 80 = 256 µg/mL). SAR analysis revealed that synthetic TZD-derivatives with substituted sulfonyl groups significantly enhanced antibacterial activity against all tested Gram-positive bacterial strains. These molecules may serve as lead compounds for developing more effective and less toxic antibacterial agents.
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JOURNAL OF COLLOID AND INTERFACE SCIENCE
·
2023
·
IF 9.9
Yu Zhang,Ruxangul Jamal,Shuyue Xie,Abdukeyum Abdurexit,Tursun Abdiryim,Yaolong Zhang,Yanyan Song,Yajun Liu
Direct methanol fuel cells (DMFCs) are thought of as portable, sustainable, and non-polluting energy devices. The exploration of efficient and affordable catalysts for the methanol oxidation reaction (MOR) is significant for the industrial application of DMFCs. In this study, nitrogen-doped hollow carbon spheres (HCS) derived from polydopamine were proposed for the catalyst support for platinum nanoparticles (Pt NPs) for serving as the anode catalyst for DMFCs, and a composite support material was fabricated by in-situ oxidation of 3,4-ethylenedioxythiophene (ProDOT) with HCS to get core-shell structured poly(3,4-propylenedioxythiophene) (PProDOT)-embellished hollow carbon spheres (HCS) (PProDOT/HCS) for further improving the catalytic activity for supported catalyst. The results indicated that the platinum (Pt) on the surface of HCS was well dispersed, and the Pt became smaller and more evenly distributed with the introduction of PProDOT. Simultaneously, the Schottky junction formed between PProDOT and Pt NPs contributes to enhanced charge transfer and catalytic activity of the catalyst. Notably, the core-shell structure of the ternary catalyst, its excellent charge transfer capability, and the interaction between platinum and the support contribute to its high electrocatalytic activity. Electrochemical tests demonstrated that the PProDOT/HCS/Pt catalyst exhibited a mass activity of 1169.6 mA mg −1 Pt for methanol oxidation in acidic electrolytes, surpassing the activity of the HCS/Pt catalyst (472.4 mA mg −1 Pt ) and commercial Pt/C (281.0 mA mg −1 Pt ).
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