中国化学快报

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Design of thiol-containing amino acids for native chemical ligation at non-Cys sites

Qiao-Qiao He, Ge-Min Fang, Lei Liu

中国化学快报. 2013, 24(04): 265-269.

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Protein chemical synthesis usually relies on the use of native chemical ligation that couples peptide thioester with a Cys-peptide. A limitation of this method is the difficulty of finding an appropriate Cys ligation site in many synthetic targets. To overcome this problem, the ligation-desulfurization approach has been developed. This approach involves the use of a thiol-containing amino acid as the ligation partner. After the sequence assembly is completed, the thiol group is removed through a desulfurization reaction to generate the standard amino acids. Currently this strategy has been applied to the ligations at a number of amino acids including Ala, Phe, Val, Lys, Thr, Leu, Pro and Gln. The present article reviews the design and synthesis of these thiol-containing amino acids for native chemical ligation at non-Cys sites.

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A μ_3-OH^- bridged two-dimensional zinc(Ⅱ) coordination polymer based on an anthryl ligand: Synthesis, characterization and luminescent properties

Jun-Jie Wanga, You-Juan Zhang, Ze Chang, Ying-Hui Zhang

中国化学快报. 2013, 24(04): 270-272.

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A two-dimensional (2D) 3,3,3,4,5,5,6-connected Zn^Ⅱ coordination compound [Zn₅(L)₂(OH)₆]_∞(L=9,10-dioxo-9,10-dihydroanthracene-1,8-dicarboxylate) has been synthesized and characterized by IR, elemental analysis, X-ray powder diffraction and single crystal X-ray diffraction analysis. Moreover, the luminescent properties of the ligand and corresponding compound have been briefly investigated.

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Neamine-heterocycle conjugates as potential anti-HIV agents

Ri-Bai Yan, Yan-Fen Wua, Jun Liu, Xiao-Lian Zhang, Xin-Shan Ye

中国化学快报. 2013, 24(04): 273-278.

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可视化

A series of neamine-heterocycle conjugates were designed and synthesized. All new compounds displayed more potent inhibitory effect on HIV replication than neamine, among them two compounds displayed stronger anti-HIV activity than neomycin B. The results suggested that itmight be a promising approach to modify neamine for the discovery of new anti-HIV agents.

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Xylyl derived oxacalixcrowns: Synthesis and crystal structure

Xiao-Yan Li, Chun Hua, Ming-Liang Maa, Yahu A. Liu, Xian-Qiang Mi, Biao Jiang, Ke Wena

中国化学快报. 2013, 24(04): 279-282.

摘要 ( )

可视化

Oxacalixcrowns 1, 2 and 3 were synthesized via reactions of dihydroxyoxacalix[2]arene[2]pyrazine 5 with ortho-, meta- and para-bis (bromomethyl) benzenes in a 1:1 fashion. The structures and conformations of 1, 2 and 3 were established by a combination of NMR, mass spectroscopies and single crystal X-ray diffraction analysis.

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“S”-shaped isopolyoxotungstate cluster decorated by calcium ions

Shuang Yao, Hong-Li Wua, Zhi-Qi Lei, Jing-Hui Yan, En-Bo Wangb

中国化学快报. 2013, 24(04): 283-286.

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One novel "S" -shaped isopolyoxotungstate Ca₂(H₂O)₁₂{Ca₄(H₂O)₁₈[H₂W₁₁O₃₇]₂}·20H₂O (1) has been successfully synthesized by the conventional aqueous solution method. Single-crystal X-ray diffraction analysis revealed that compound 1 crystallized in triclinic system, space group P_-1, with lattice constants a=12.591(3)Å, b=12.738(3)Å , c=17.961(4)Å, α=98.97(3)°, β=99.85(3)°, γ=93.42(3)°. The "S"-shaped cluster was built from two {W₁₁} subunits, four Ca₂₊ linking units and two {Ca(H2O)6}2+ decorating fragments. The electrochemical properties of 1 have been investigated in details.

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A novel and simple pathway to synthesis of porous polyurea absorbent and its tests on dye adsorption and desorption

Shu-Sheng Li, Xiang-Zheng Kong, Xu-Bao Jiang, Xiao-Li Zhu

中国化学快报. 2013, 24(04): 287-290.

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A novel one-step protocol for the preparation of porous polyurea material (PPU) through precipitation polymerization of toluene diisocynate (TDI) is presented. The process is based on step polymerization of one singlemonomer, TDI, with water in water-acetonemixed solvent. PPU is obtained without need for any porogen or additives, and no any chemical modification on the outcome polymer is necessary. The morphology, pore size and size distribution of PPU are characterized by scanning electron microscope and BET nitrogen adsorption. Taking acid fuchsine (AF) and Congo Red as dye examples in wastewaters, their adsorption on, desorption from PPU and the reusability of PPU were tested. Experimental conditions for AF adsorption were optimized with regard to pH, adsorption time, AF concentration and amount of PPU. Results demonstrate that the as-prepared PPU is of high performance in dyes adsorption and recycled use. This work presents therefore a novel and attractive candidate for removal of anionic dyes from wastewaters.

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Phenylboronic acid and dopamine as probe set for electrochemical detection of saccharides

Jian Li, Ya-Qin Sun, Yin-Mao Wei, Jian-Bin Zheng

中国化学快报. 2013, 24(04): 291-294.

摘要 ( )

可视化

A novel electrochemical approach for detection of saccharides via indicator displacement assay was presented. In this system, 2-fluorophenylboronic acid and dopamine (DA) were performed as probe set. The electrochemical properties of DA and the binding to 2-fluorophenylboronic acid in phosphate buffer at different pH values were investigated by cyclic voltammetry. After addition of fructose to the solution, a competition for the binding 2-fluorophenylboronic acid occurred that led to the release of the DA. The regenerate oxidation current of DA increased with increasing fructose concentration. Under optimized experimental conditions, the peak current was linearly related to fructose concentration in the range of 0.3-5.0 mmol/L with a detection limit of 0.1 mmol/L. In addition, the interaction between 2-fluorophenylboronic acid and other cis-diol compounds such as glucose, galactose and mannose was investigated.

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Scaffold-hopping strategy toward calanolides with nitrogen-containing heterocycles

Xiao-Yong Guo, Gang Liu

中国化学快报. 2013, 24(04): 295-298.

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(+)-Calanolide A was the first natural product identified as an active agent against HIV-1 and Mycobacterium tuberculosis (Mtb). In devising a scaffold-hopping strategy of structure modification of (+)-calanolide A, we focused on the synthesis of calanolides by replacing ring D with various five or six membered nitrogen-containing heterocycles, hoping to get further understanding of the structure- activity relationship.

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Synthesis and cytotoxic evaluation of new colchicine derivatives bearing 1,3,4-thiadiazole moieties

Li-Hong Shen, Hong-Yu Li, Hui-Xia Shang, Shu-Ting Tian, Yi-Sheng Lai, Li-Jie Liu

中国化学快报. 2013, 24(04): 299-302.

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In search of novel anticancer agents, a series of N-methyl colchiceinamide derivatives (7a-7i) containing 1,3,4-thiadiazole moieties were synthesized, and their structures were confirmed by spectral analysis. Cytotoxicity of these compounds was evaluated by MTT assay in vitro against four human tumor cell lines, i.e. A2780, A549, BEL7402, and MCF-7. The results indicated that most of the derivatives showed significant anticancer activities, particularly, compounds 7h and 7i showed more potent cytotoxic activities of all screened cancer cells than colchicine.

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Design and synthesis of novel antifungal triazole derivatives with good activity and water solubility

Xu-Feng Cao, Wen-Jing Chu, Yong-Bing Cao, Yu-She Yang

中国化学快报. 2013, 24(04): 303-306.

摘要 ( )

可视化

In order to find novel antifungal agents with good activity and aqueous solubility, a series of SYN-2869 analogues containing a pyridine ring were synthesized and evaluated for their in vitro antifungal activity and water solubility. The results indicated that some compounds showed potent activity against six pathogenic fungi. In particular, the analogue 17a having an isobutyl substitution on the triazolone exhibited significant broad spectrum antifungal activity. In addition, the water solubility of compound 17a was sufficiently improved over SYN-2869.

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Effects of Mo promoters on the Cu-Fe bimetal catalysts for the DMC formation from CO₂ and methanol

Ying-Jie Zhou, Min Xiao, Shuan-Jin Wanga, Dong-Mei Han, Yi-Xin Lu, Yue-Zhong Meng

中国化学快报. 2013, 24(04): 307-310.

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可视化

The Mo-promoted Cu-Fe bimetal catalysts were prepared and used for the formation of dimethyl carbonate (DMC) from CO₂ and methanol. The catalysts were characterized by X-ray diffraction (XRD), temperature programmed reduction (TPR), laser Raman spectra (LRS), energy dispersive spectroscopy (EDS) and temperature programmed desorption (TPD) techniques. The experimental results demonstrated that the Mo promoters can decrease the reducibility and increase the dispersion of Cu-Fe clusters. The concentration balance of base-acid sites can be readily adjusted by changing the Mo content. The moderate concentration balance of acid and base sites was in favor of the DMC formation. Under optimal experimental conditions, the highest methanol conversion of 6.99% with a DMC selectivity of 87.7% can be obtained when 2.5 wt% of Mo was loaded.

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Determination of trace level of perchlorate in Antarctic snow and ice by ion chromatography coupled with tandem mass spectrometry using an automated sample on-line preconcentration method

Su Jiang, Yuan-Sheng Li, Bo Sun

中国化学快报. 2013, 24(04): 311-314.

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可视化

A new ion chromatography coupled with tandem mass spectrometry (IC-ESI-MS/MS) method, with automated sampling and on-line preconcentration, has been developed for the determination of perchlorate in Antarctic snow and ice at low part-per-trillion (ng/L) levels. To the best of our knowledge, this is the first time that an analytical method is used for the determination of perchlorate in Antarctic snow and ice. The IC-ESI-MS/MS instrumentation consisted of an ICS2000 ion chromatography (IC) system coupled to an API3200 electrospray tandem mass spectrometer (ESI-MS/MS). On-line preconcentration was realized through a six-port injector valve, a TAC-ULP1 concentrator column and an AS auto-sampler. Multiple reaction monitoring (MRM) mode was used to quantify the perchlorate anion. The transition of ³⁵Cl¹⁶O₄^-(m/z 98.9) into ³⁵Cl¹⁶O₃^-(m/z 82.9) was monitored for quantifying the main analyte, and the transition of ³⁷Cl¹⁶O₄ (m/z 100.9) into ³⁷Cl¹⁶O₃^-(m/z 84.9) was monitored for examining a proper isotopic abundance ratio of ³⁵Cl to ³⁷Cl, which was used as a confirmation tool. The limit of detection (LOD) and limit of quantitation (LOQ) for the method was 0.2 ng/ L and 0.5 ng/L, respectively. And this new method exhibited acceptable accuracy and precision for samples at ng/L levels. All the tested snow and ice samples were found to contain measurable amount of perchlorate, ranging from 10 ng/L to 340 ng/L.

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Potentiometric determination of mefenamic acid in pharmaceutical formulation by membrane sensor based on ion-pair with basic dye

Zholt Kormosh, Oksana Matviychuk

中国化学快报. 2013, 24(04): 315-317.

摘要 ( )

可视化

The characteristics, performance and application ofmembrane sensors based on ion-pair Brilliant Green mefenamate are described. The sensor's response to the mefenamate ion has the sensitivity of (86.0±2.0) mV/pC over the range of 9×10^-5-1×10^-2 mol/L and the detection limit of 4.5×10^-5mol/L at pH 8.5-12. The sensor is easily assembled at a relatively low cost and has fast response time (5-10 s). The proposed sensor displayed good selectivity for mefenamate ion in the presence of different substances. It was used to determine mefenamic acid in pharmaceuticals.

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Simple route to indeno[1,2-b]quinoline derivatives via a coupling reaction catalyzed by TiO₂ nanoparticles

Shahrzad Abdolmohammadi

中国化学快报. 2013, 24(04): 318-320.

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可视化

A simple, efficient and high yielding approach for the synthesis of indeno[1,2-b]quinolinediones has been developed by a one-pot, four-component, coupling reaction utilizing TiO₂ nanoparticles (TiO₂-NPs) as a heterogeneous catalyst at 80℃ in aqueous media.

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Synthesis, pharmacokinetics and in vivo antifungal activity of the novel water-soluble prodrugs of itraconazole analogue YL-24

Yu Liu, Xu-Feng Cao, Xin Liu, Yong-Bing Cao, Wen-Jing Chu, Yu-She Yang

中国化学快报. 2013, 24(04): 321-324.

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可视化

To improve the aqueous solubility of an itraconazole analogue, compound 1 (YL-24), a series of novel prodrugs were synthesized. Among these prodrugs, the phosphate disodium salt compound 7 exhibited excellent aqueous solubility (9.8 mg/mL) at near-neutral pH and sufficient stability in buffer solutions, along with favorable pharmacokinetic profiles. In particular, compounds 1 and 7 provided moderate survival efficacy in murine systemic Candida albicans SC5314 infection model, but their efficacy was weaker than that of fluconazole.

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Synthesis and bioactivities of some new 1H-pyrazole derivatives containing an aryl sulfonate moiety

Babasaheb V. Kendre, Mahadev G. Landge, Wamanrao N. Jadhav, Sudhakar R. Bhusare

中国化学快报. 2013, 24(04): 325-328.

摘要 ( )

可视化

A new series of 1H-pyrazole derivatives 5a-j bearing an aryl sulfonatemoiety have been synthesized by a one-pot cyclo-condensation reaction of 2-(3-(dimethylamino)acryloyl)phenyl-4-methyl benzene sulfonates 4a-e and hydrazine hydrate or phenyl hydrazine in ethanol under reflux conditions. Some of the newly synthesized compounds were screened for their anti-inflammatory activity. All synthesized compounds were screened against Gram positive and Gram negative bacterial and fungal strains. The compound 5b was found to be a potent anti-inflammatory agent while the majority of the compounds were found to be active against microbial strains.

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Electrochemical study of sulfadiazine on a novel phthalocyanine-containing chemically modified electrode

Xiao-Ping Hong, Jing-Ying Ma

中国化学快报. 2013, 24(04): 329-331.

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In this paper, cobalt tetraaminophthalocyanine (CoPc) was successfully deposited onto a carbon nanotubes modified electrode by consecutive cyclic scanning in supporting electrolyte containing CoPc to form phthalocyanine-containing chemically modified electrode. The electrochemistry of sulfadiazine was studied by voltammetric method and flow injection analysis at the new modified electrode. Compared with glassy carbon electrode, the new modified electrode exhibited exciting performance including low oxidation potential, high current response and promising flow injection response.

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Rapid and sensitive detection of pesticides by surface-enhanced Raman spectroscopy technique based on glycidyl methacrylate-ethylene dimethacrylate (GMA-EDMA) porous material

Qing-Qing Li, Yi-Ping Dua, Ying Xu, Xuan Wanga, Shi-Qian Maa, Jin-Pei Geng, Peng Cao, Tao Sui

中国化学快报. 2013, 24(04): 332-334.

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A novelmethod of fast and sensitive SERS detection using GMA-EDMA porous material combined with a miniature device was reported in this study. A 100 μL solution containing sample, silver colloid and NaCl was evenly mixed to ensure the sample molecules would adsorb onto silver nanoparticles. Then the mixture was added onto the porous material surface slowly, so that the aggregation of silver colloid would stay on the surface while the liquid components would flow away. This technology can improve the sensitivity of SERS detection. By this method, two pesticides tricyclazole and paraquat were successfully detected at concentrations of 5×10^-3 mg/L and 1×10^-3 mg/L, respectively.

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Preparation and characterization of optically functional hollow sphere hybrid materials by surface-initiated RATRP and “click” chemistry

Xin-Hu Lv, Li-Ping Wang, Guang Li, Xue-Xi Gao, Pan-Pan Pan, Li-Mei Zhang

中国化学快报. 2013, 24(04): 335-337.

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The randomcopolymers grafted onto the surfaces of SiO₂ hollow sphere via reverse atom transfer radical polymerization (RATRP) and "click" chemistry were investigated. A sufficient amount of peroxides, as initiating moieties, were introduced onto the surface of hollow spheres. Then styrene and 4-vinylbenzyl azide were polymerized via surface-initiated reverse atom transfer radical polymerization (SI-RATRP) using the peroxide group modified hollow sphere as initiator, resulting in hollow spheres (HS) with grafted polystyrene-co-poly(4-vinylbenzyl azide) copolymer brushes as (HS-g-PS-co-PVBA) intermediate material. Subsequently, N-propargyl-carbazole (PC) was covalently bonded to HS-g-PS-co-PVBA by the "click" reaction, resulting in the HS-g-PS-co-PVBPC hybrid material. The excitation spectrum is dominated by a broad band from 350 nmto 400 nmwith the maximum peak at 362 nm, attributed to the characteristic absorption of the carbazole group of HS-g-PS-co-PVBPC hybrid material.

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Synthesis and physiochemical property evaluation of carbamate derivatives of scutellarin methyl ester

Feng-Jie Jiang, Xiao-Zhong Fu, Shan-Wu Wang, Yong Huang, Wen Zhou, Ai-Min Wang, Yong-Lin Wang

中国化学快报. 2013, 24(04): 338-340.

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可视化

A series of carbamate prodrugs of scutellarin methyl ester (4a-4e) were prepared in the presence of bis(trichloromethyl) carbonate (BTC) with scutellarin methyl esters and L-amino acid tert-butyl ester hydrochloride as starting materials. In vitro stability and aqueous solubility of target compounds were evaluated. The results indicated that compounds 4d and 4e have higher solubility and in vitro stability than scutellarin respectively.

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β-Cyclodextrin assisted one-pot synthesis of mesoporous magnetic Fe₃O₄@C and their excellent performance for the removal of Cr (Ⅵ) from aqueous solutions

Hui Zhang, De-Lei Liu, Li-Li Zeng, Meng Li

中国化学快报. 2013, 24(04): 341-343.

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可视化

Mesoporous magnetic Fe₃O₄@C nanoparticles have been synthesized by a one-pot approach and used as adsorbents for removal of Cr (Ⅳ) from aqueous solution. Magnetic iron oxide nanostructured materials encapsulated by carbon were characterized by scanning electron microscope (SEM), nitrogen adsorption and desorption, X-ray diffraction (XRD) and Fourier transform infrared (FTIR) spectroscopy. The adsorption performance of the nanomaterial adsorbents is tested with the removal of Cr (Ⅳ) from aqueous solution. The results reveal that the mesoporous magnetic Fe₃O₄₃O₄3O₄@C exhibited 1.8 times higher removal rate of Cr (Ⅵ). Themesoporous structure and an abundance of hydroxy groups on the carbon surfacemay be responsible for high absorbent capability.

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Enhanced catalytic features of sol-gel immobilized MnP isolated from solid state culture of Pleurotus ostreatus IBL-02

Muhammad Asgher, Hafiz Muhammad Nasir Iqbal

中国化学快报. 2013, 24(04): 344-346.

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可视化

An indigenous and industrially important manganese peroxidase (MnP) isolated from solid state culture of Pleurotus ostreatus IBL-02 was 2.1-fold purified and immobilized using sol-gel matrix of trimethoxysilane and proplytetramethoxysilane. Lower K_M, higher V_max, hyper-activation, enhanced acidic and thermal stability up to 70℃, were the improved/enhanced catalytic features of the presently sol-gel immobilized MnP. A maximum of 100% decolorization was achieved within a short time period for the different real dyes containing textile industry effluents i.e. Nishat textile (NIT), K&N textile (KIT), Sitara textile (SIT), and Crescent textile (CRT).

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An efficient synthesis of 2,3-diaryl-2-azabicyclo[2.2.2]octan-5-ones and their acetylcholinesterase inhibitory activity

Li Huang, Jun-Pei Chen, Can Jin, Wei-Ke Su

中国化学快报. 2013, 24(04): 347-350.

摘要 ( )

可视化

A series of substituted 2,3-diaryl-2-azabicyclo[2.2.2]octan-5-ones have been prepared by an efficient three-component aza-Diels-Alder cycloaddition reaction in water catalyzed by layered α-zirconium hydrogen phosphate (α-ZrP) and sodium calix[4]arene sulfonates bearing pendant short aliphatic chains. The 18 synthesized compounds were assayed for acetylcholinesterase inhibition using mouse acetylcholinesterase.

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2013年, 第24卷, 第04期　刊出日期：2013-04-20

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2013年, 第24卷, 第04期 刊出日期：2013-04-20

2013年, 第24卷, 第04期　刊出日期：2013-04-20