EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
·
2023
·
IF 6.7
Cong Chen,Bing Zhang,Jiaojiao Tu,Yanfen Peng,Yihuan Zhou,Xinping Yang,Qiming Yu,Xiangduan Tan
Farnesoid X receptor (FXR) plays a key role in bile acid homeostasis , inflammation, fibrosis , lipid and glucose metabolism and is emerging as a promising therapeutic target for nonalcoholic steatohepatitis (NASH). Emerging evidence suggested that intestine-specific FXR antagonists exhibited remarkable metabolic improvements and slowed NASH progression. In this study, we discovered several potent FXR antagonists using a multistage ligand- and structure-based virtual screening approach. Notably, compound V023-9340 , which possesses a 4-aminophenylacetamide scaffold, emerged as the most potent FXR antagonist with an IC 50 value of 4.27 μM. In vivo , V023-9340 demonstrated selective accumulation in the intestine, substantially ameliorating high-fat diet (HFD)-induced NASH in mice by mitigating hepatic steatosis and inflammation. Mechanistic studies revealed that V023-9340 strongly inhibited intestinal FXR while concurrently feedback-activated hepatic FXR. Further structure-activity relationship optimization employing V023-9340 has resulted in the synthesis of a more efficacious compound V02-8 with an IC 50 value of 0.89 μM, which exhibited a 4.8-fold increase in FXR antagonistic activity compared to V023-9340 . In summary, 4-aminophenylacetamide derivative V023-9340 represented a novel intestine-specific FXR antagonist and showed improved effects against HFD-induced NASH in mice, which may serve as a promising lead in discovering potential therapeutic drugs for NASH treatment.
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高影响因子
JOURNAL OF LUMINESCENCE
·
2023
·
IF 3.6
Ruiqi Yang,Ju Li,Xinjing Xie,Jingjing Lian,Chaoyue Wang,Changlin Li,Haoran Su,Zhequan Zou,Shouan Xie,Ruijin Yu
In this study, a series of innovative red-emitting Sm 3+ -doped K 5 La(MoO 4 ) 4 phosphors were synthesized using the solid-state reaction method. The X-ray powder diffraction patterns and Rietveld refinement confirmed the single-phase structure of the synthesized K 5 La(MoO 4 ) 4 :Sm 3+ samples with trigonal system (space group R 3 ‾ m (#166)). The phosphors demonstrated a strong red emission at 644 nm, corresponding to the electric dipole transition 4 G 5/2 → 6 H 9/2 of Sm 3+ ions. The optimal doping concentration for K 5 La (1- x ) ( MoO 4 ) 4 : x Sm 3+ was found to be approximately 5 mol%. The temperature-dependent emission of phosphors was examined and found that the luminescence intensity remained at 86 % even at 480 K, showing the exceptional thermal stability of this material. K 5 La (1- x ) ( MoO 4 ) 4 : x Sm 3+ phosphors displayed remarkable color stability with chromaticity coordinates falling within the red region in 1931 CIE diagram. K 5 La(MoO 4 ) 4 :5 mol%Sm 3+ exhibited a high color purity of 99.9 % and internal quantum efficiency (IQE) was measured as 66.8 %. Light-emitting diodes (LEDs) were constructed using InGaN chips and the synthesized red phosphors. The chromaticity coordinates of the fabricated w-LED (white light-emitting diode) were (0.330, 0.351), closely resembling the typical white point of the National Television System Committee (NTSC) at (0.333, 0.333). The color rendering index (CRI, R a ) and correlated color temperature (CCT) of w-LED were 87 and 5627 K. These findings strongly suggest the potential use of K 5 La(MoO 4 ) 4 :Sm 3+ phosphors as red phosphors in LEDs.
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ACS Applied Nano Materials
·
2023
·
IF 5.9
Xiaoqiu Yao,Ming Jin,Jiang Du,Decheng Wan
In the jigsaw puzzle of quality gold nanoclusters (AuNCs), those protected by weak ligands or coligands are still rarely available. Here, we provide an example in the case of supported AuNCs. Branched polyethylenimine (PEI, diameter of 1.86 nm) is introduced as discrete molecular patches onto the support of mesoporous polymer beads. Each patch is derived into polyaminophosphine with 2-(diphenylphosphino) benzaldehyde (dppb). The molecular patch is of nanoscale and uniform size. The polymer beads after PEI loading bear unimodal pores (3.9 nm), and the specific surface area is of 390 m2 g–1. AuNCs are obtained by mildly heating the mixture of the functionalized beads and aqueous chloroauric acids. Uniform AuNCs with a diameter of 1.2 ± 0.2 nm (∼53 Au atoms) are obtained when each PEI patch bears 17 dppb ligands, smaller than that of 3.5 nm in the absence of any dppb, suggesting that dppb enhances the nucleation of AuNCs. The heteroleptic AuNCs show ultrahigh catalytic performance (TOF = 391 h–1) for the reduction of 4-nitrophenol, where the dppb ligands hardly suppress the catalytic activity. The catalyst is well recoverable and durable for the reduction of 4-nitrophenol.
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ORGANIC PROCESS RESEARCH & DEVELOPMENT
·
2023
·
IF 3.4
Junjie Li,Wei Feng,Shichun Weng,Zichao Guo,Wanghua Chen
3,4-bis(4-Aminofurazano-3-yl) furoxan (DATF) is a key precursor for the high-energy explosive 3,4-bis(4-nitrofurazano-3-yl) furoxan (DNTF), and it is also a high-nitrogen content energetic material. In this paper, the synthesis process of DATF was characterized using the HPLC technique, and the effects of four reaction parameters have been thoroughly studied. The thermal risk analysis for DATF synthesis was conducted with a reaction calorimeter (RC1) and an accelerating rate calorimeter. It was found that extracting the intermediate 3-amino-4-oxycyanofurazan from the aqueous to organic phases was an important way to improve the yield of DATF. Therefore, hydrophobic ethyl acetate was selected as one reaction solvent. The higher yield of DTAF obtained was about 60%. In addition, HPLC monitoring and reaction calorimetry results indicated that the rate of diazotization and decomposition of diazonium salt was feeding-controlled, and the cycloaddition reaction was a slow process. Most of the reaction heat has been released by the diazotization and decomposition of diazonium salt, while the heat effect of cycloaddition was not significant. Thermal stability analysis supported the conclusion that the decomposition of the reaction mixture was hardly possible to be triggered by the reaction heat. The thermal risk of DATF synthesis was low.
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Molecular Catalysis
·
2023
·
IF 4.6
Yuanning Yue,Ying Liao,Jiarong Lu,Yue Pan,Meiyu Zhang,Guiyue Chen,Xin Zhou,Xinyu Kuang,Hui Zhao,Xiaobo Chen,Xiang Feng,Hao Yan,Yibin Liu,Chaohe Yang
Recognizing and modifying the acid property-dependent catalytic characteristics of catalysts are of great importance for Prins condensation reaction. Herein, a series of metal-doped M-NH 4 -PW catalysts ( M =Pt, Fe, Ir, Ru) are successfully synthesized for Prins condensation reaction of formaldehyde and propylene to produce 4-methyl-1,3-dioxane. Our findings demonstrate that the catalytic performance of M-NH 4 -PW catalysts is influenced by the chemical nature of metal site properties with different electron transfer abilities. Specifically, the new Lewis acid decorated by Pt metal on 4-H site is more favorable for the selective adsorption of formaldehyde and activation of its C O bond. Additionally, the synergistic effect between Pt metal sites and nearby O in [PW 12 O 40 ] 3− promotes the formation of C C bonds between protonated formaldehyde and propylene. Consequently, the Pt-NH 4 -PW catalyst exhibits high conversion (> 80 %) and simultaneous selectivity towards 4-methyl-1,3-dioxane selectivity (65 %). This strategy may provide valuable insights for developing efficient multifunctional catalysts for Prins condensation reactions.
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MAIN GROUP CHEMISTRY
·
2020
·Vol. 19
·期 3
·227-235
·
IF 0.845
Lu Yan-Qi
A new hybrid compound consisting of 1,4-bis(4-pyridylthio)butane ([Bpytb]) ligand, namely {[Bpytb]Ag2I3}n (1), has been prepared and characterized by IR spectroscopy, solid UV-visible diffuse reflectance spectrum, X-ray Powder Diffraction (PXRD) and TG. Compound 1 consists of 1D anion chain structure. Crystal system: Monoclinic, Space group: P2/c, a = 4.5092(3), b = 11.1895(9), c = 21.3893(14), α= 90°, β= 92.907(2)°, γ= 90°, V = 1077.82(13) Å3, Z = 2, Dcalc = 2.693 g cm–3. The photocatalytic property of compound 1 was also studied and it exhibits a better degradation effect on organic dye MB.
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JOURNAL OF MOLECULAR LIQUIDS
·
2017
·
IF 3.648
Chen Yang,Qi Li,Yong Wu
Data on corresponding solid-liquid equilibrium of 4-methylbenzoic acid in different solvents are essential for a preliminary study of industrial applications. In this paper, the solid-liquid equilibrium of 4-methylbenzoic acid in methanol, ethanol, isopropanol, 1-butanol, acetone and acetonitrile pure solvents and (acetone + acetonitrile) mixture solvents were explored in the temperatures (from 278.15 to 323.15 K) under atmosphere pressure. For the temperature range investigated, the solubility of 4-methylbenzoic acid in the solvents increased with increasing temperature. The modified Apelblat model, the Buchowski-Ksiazaczak λh model, and the ideal model were adopted to describe and predict the change tendency of solubility. Computational results showed that the modified Apelblat model had more advantages than the other two models. The solubility data were fitted using a modified Apelblat equation, a variant of the combined nearly ideal binary solvent/Redich-Kister (CNIBS/R-K) model, Jouyban-Acree model and Ma model in (acetone + acetonitrile) binary solvent mixture. In addition, the calculated thermodynamic parameters indicated that in each studied solvents the dissolution of 4-methylbenzoic acid is endothermic and entropy-driven process.
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FOOD CONTROL
·
2023
·
IF 6
Lingling Yu,Xingxing Wang,Yingying Wei,Shu Jiang,Jianfen Ye,Yi Chen,Feng Xu,Hongfei Wang,Xingfeng Shao
Terpinen-4-ol has potent antifungal activity and controls decay in postharvest strawberry fruit. In order to overcome the unstable and volatile characteristics of terpinen-4-ol, a γ-cyclodextrin (γ-CD) metal-organic framework (MOF) with high porosity and large specific surface area was synthesized by vapor diffusion and ultrasonic mixing. Terpinen-4-ol-loaded γ-CD-MOF (γ-CD-MOF/Ter) was then prepared using physical adsorption. Scanning electron microscopy, X-ray diffraction, Fourier transform infrared spectroscopy analysis, and nitrogen adsorption-desorption showed that terpinen-4-ol was successfully loaded into the center of the γ-CD-MOF structure, and that encapsulation efficiency and drug loading reached 53.61% and 9.31%, respectively. γ-CD-MOF/Ter reduced the release rate of terpinene-4-ol, and exhibited the higher antifungal effect against B. cinerea in vitro test. Meanwhile, it was effective in controlling gray mold and maintaining the quality of strawberry fruit. We conclude that γ-CD-MOF loads terpinen-4-ol and reduces its volatilization and has potential application in the preservation of strawberry fruit.
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CERAMICS INTERNATIONAL
·
2023
·
IF 5.2
Gang Li,Ruiyang Tan,Xiangcheng Lu,Xinyu Zhang,Chengcheng Zhang,Bohong Gao,Yuting Zhou,Ke Chen,Ping Chen,Xinyi Wang
Chemical composition and morphological optimization are both effective strategies for constructing excellent electromagnetic wave absorption (EMWA) materials. While efficient EMWA materials derived from both metal-organic frameworks (MOFs) and MXenes have been extensively studied, composites derived from the Hofmann framework with MXene have not been reported. In this study, we employed a Hofmann framework ([Fe(pz)Ni(CN) 4 ], pz = pyrazine) and MXene (Ti 3 C 2 T x ) to create new MXene@Hofmann (MH1 and MH2) composites, using a simple co-precipitation method with two different contents of [Fe(pz)Ni(CN) 4 ]. The FeNi/C/TiO 2 composites with a multi-layered structure inherited from MXene were prepared by annealing the MXene@Hofmann composites at 500, 600, and 700 °C, resulting in the formation of MH1-500/600/700 and MH2-500/600/700 composites. Their compositions, morphologies, electromagnetic parameters, and EMWA performances were characterized. For the composites with a high [Fe(pz)Ni(CN) 4 ] content, MH2-600 has a minimum reflection loss ( RL min ) value of −30.63 dB at a thickness of only 1.8 mm and the broadest effective absorption bandwidth (EAB) of 3.90 GHz at 2.0 mm, while MH2-700 exhibits superior EMWA performance with an RL min value of −34.34 dB at 1.9 mm and an EAB value of 4.96 GHz at 2.1 mm. Their impressive EMWA performance might be attributed to the synergistic dielectric loss and magnetic loss and also the impedance matching from the reasonable ratio of the magnetic and dielectric components. This work demonstrates an effective strategy for constructing EMWA materials from the Hofmann framework and MXene.
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高影响因子
ADVANCED FUNCTIONAL MATERIALS
·
2023
·Vol. 33
·期 44
·2304237
·
IF 19
Dongfang Xu,Jungang Wang,Yuwei Duan,Shaomin Yang,Hong Zou,Lu Yang,Na Zhang,Hui Zhou,Xuruo Lei,Meizi Wu,Shengzhong Liu,Zhike Liu
The poor interface quality between cesium lead triiodide (CsPbI 3 ) perovskite and the electron transport layer limits the stability and efficiency of CsPbI 3 perovskite solar cells (PSCs). Herein, a 4-amino-2,3,5,6-tetrafluorobenzoate cesium (ATFC) is designed as a bifacial defect passivator to tailor the perovskite/TiO 2 interface. The comprehensive experiments demonstrate that ATFC can not only optimize the conductivity, electron mobility, and energy band structure of the TiO 2 layer by passivation of the undercoordinated Ti 4+ , oxygen vacancy ( V O ), and free OH defects but also promote the yield of high-quality CsPbI 3 film by synergistic passivation of undercoordinated Pb 2+ defects with the CO group and F atom, and limiting I − migration via F···I interaction. Benefiting from the above interactions, the ATFC-modified CsPbI 3 device yields a champion power conversion efficiency (PCE) of 21.11% and an excellent open-circuit voltage ( V OC ) of 1.24 V. Meanwhile, the optimized CsPbI 3 PSC maintains 92.74% of its initial efficiency after aging 800 h in air atmosphere, and has almost no efficiency attenuation after tracking at maximum power point for 350 h.
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PROCESS BIOCHEMISTRY
·
2023
·
IF 4.4
Haidong Teng,Kaitong Chen,Lan Wang,Jianping Wu,Gang Xu
l -syn-3-[4-(methylsulfonyl)] phenylserine is a key industrial intermediate for the synthesis of florfenicol, thiamphenicol , and other products. l -Threonine aldolase can synthesize l -syn-3-[4-(methylsulfonyl)] phenylserine from glycine and 4-methylsulphonyl benzaldehyde directly. However, the selectivity of free l -threonine aldolase was difficult to meet the requirement of industrialization. Here, we selected the suitable site to insert His tag as immobilized site to improve the selectivity of l -threonine aldolase based on the molecular dynamics simulation and prior protein engineering. The phenanthroline was coupled to the surface of magnetic nanoparticles coated with silicon and thus enabled the selective and oriented immobilization of His-tagged l -threonine aldolase. Due to magnetic nanoparticles coated with silicon as supports, it was easy to separate the residual reactant and impurities from the immobilized enzyme by magnetic attraction. Moreover, the immobilization was combined with the purification of free enzymes through directional immobilization, which avoided heterozyme linking supports and improved the utilization efficiency of supports. Our study demonstrates an effective approach: how to analyze and select enzyme-targeted ligation sites in conjunction with previous modifications of engineered bacteria, and the immobilized enzyme obtained also provided a good candidate for the industrial production of l -syn-3-[4-(methylsulfonyl)] phenylserine.
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EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
·
2023
·
IF 6.7
Yong-Jun Huang,Xiao-Lin Zhong,Yi-Peng Zang,Ming-Han Yang,Jing Lin,Wei-Min Chen
The natural prenylated chalcone isobavachalcone ( IBC ) shows good antibacterial activity against Gram-positive bacteria but is ineffective against Gram-negative bacteria, most likely due to the outer membrane barrier of Gram-negative bacteria. The Trojan horse strategy has been shown to be an effective strategy to overcome the reduction in the permeability of the outer membrane of Gram-negative bacteria. In this study, eight different 3-hydroxy-pyridin-4(1 H )-one-isobavachalcone conjugates were designed and synthesized based on the siderophore Trojan horse strategy. The conjugates exhibited 8- to 32-fold lower minimum inhibitory concentrations (MICs) and 32- to 177-fold lower half-inhibitory concentrations (IC 50 s) against Pseudomonas aeruginosa PAO1 as well as clinical multidrug-resistant (MDR) strains compared to the parent IBC under iron limitation. Further studies showed that the antibacterial activity of the conjugates was regulated by the bacterial iron uptake pathway under different iron concentration conditions . Studies on the antibacterial mechanism of conjugate 1b showed that it exerts antibacterial activity by disrupting cytoplasmic membrane integrity and inhibiting cell metabolism. Finally, conjugate 1b showed a lower cytotoxic effects on Vero cells than IBC and a positive therapeutic effect in the treatment of bacterial infections caused by Gram-negative bacteria PAO1. Overall, this work demonstrates that IBC can be delivered to Gram-negative bacteria when combined with 3-hydroxy-pyridin-4(1H)-ones as siderophores and provides a scientific basis for the development of effective antibacterial agents against Gram-negative bacteria.
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