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Convenient one-pot synthesis and biological evaluation of phosphoramidates and phosphonates containing heterocycles 含杂环磷酰胺酸盐和磷酸盐的便捷一锅合成及生物学评价
Pub Date : 2018-03-14 DOI: 10.1080/10426507.2018.1452229
Sk. Nayab Rasool, Ch. Subramanyam, D. B. Janakiramudu, P. Supraja, R. Usha, C. N. Raju
GRAPHICAL ABSTRACT ABSTRACT A series of new phosphoramidates and phosphonates were synthesized in single step by reacting diethyl phosphorochloridate with various bioactive amines. The newly synthesized compounds 3a-j were tested for antibacterial activity against Gram-positive and Gram-negative bacteria. All the title compounds exhibited good activity. Amongst all the tested compounds, 3b (diethyl(4-(6-fluorobenzo(d)isoxazol-3-yl)piperidin-1-yl)phosphonate), 3c (diethyl 4, 6-difluorobenzo(d)thiazole-2-ylphosphoramidate) and 3d (diethyl 5-nitro-1H-indazol-1-yl- phosphonate) displayed promising antimicrobial activity against Pseudomonas aeruginosa and Trichoderma viride due to the presence of electron with drawing fluoro and nitro groups respectively.
摘要以多种生物活性胺为原料,以氯化磷二乙酯为原料,一步合成了一系列新的磷酸酯和膦酸盐。对新合成的化合物3a-j进行了对革兰氏阳性菌和革兰氏阴性菌的抑菌活性测试。标题化合物均表现出良好的活性。在所有被测试的化合物中,3b(二乙基(4-(6-氟苯并(d)异恶唑-3-基)哌啶-1-基)膦酸盐)、3c(二乙基4,6 -二氟苯并(d)噻唑-2-基磷酰胺)和3d(二乙基5-硝基-1-吲哚-1-基膦酸盐)由于分别存在带氟和硝基的电子而对铜绿假单胞菌和绿木霉表现出良好的抗菌活性。
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引用次数: 9
Synthesis of polycyclic mixed phenothiazine-phenoxazine organic dyes 多环混合吩噻嗪-吩恶嗪有机染料的合成
Pub Date : 2018-03-06 DOI: 10.1080/10426507.2018.1436545
Efeturi A. Onoabedje, Obioma Chinwe Chinwuko, B. Ezema, M. A. Ezeokonkwo
GRAPHICAL ABSTRACT ABSTRACT A convenient synthesis of new polycyclic mixed phenothiazine-phenoxazine compounds is described. The cross-coupling of 2,4-diaminothiophenol with 2,3-dichloro-1,4-naphthoquin one at room temperature gave reddish brown 10-amino-6-chlorobenzo[a]phenoxazin-5-one which was converted into a benzoxazinophenothiazin-12-amine in 58% yield via reaction with 2-aminothiophenol under anhydrous basic conditions. A three-component one-pot synthesis improved the yield of benzoxazinophenothia-12-amine to 81% a in shorter time compared to two steps reactions. The synthesis of new azomethine derivatives of benzo[a]benzo[5,6] [1,4] oxazino [3,2-c] phenothiazin-12-amine with extended conjugations and excellent yields were also reported. The structural assignments of the prepared compounds were established by combine Ultraviolet-Visible, Fourier Transform Infrared, 1H and 13C Nuclear Magnetic Resonance Spectroscopies, Mass Spectrometry and elemental analytical data. The ease of preparations in high yields and their intense colourations make these compounds applicable as dyestuffs.
摘要描述了一种新的多环混合吩噻嗪-吩恶嗪化合物的简便合成方法。2,4-二氨基噻吩与2,3-二氯-1,4-萘醌在室温下交叉偶联得到红棕色的10-氨基-6-氯苯并[a]苯恶嗪-5- 1,并与2-氨基噻吩在无水碱性条件下以58%的收率合成苯并恶嗪-12-胺。与两步反应相比,采用三组分一锅法合成苯并恶嗪-12-胺的产率可在较短的时间内达到81%。本文还报道了苯并[a]苯并[5,6][1,4]恶氮杂氮[3,2-c]吩噻嗪-12-胺的扩展偶联衍生物的合成,并取得了优异的产率。通过紫外可见光谱、傅里叶变换红外光谱、1H和13C核磁共振光谱、质谱和元素分析数据确定了化合物的结构。制备容易,产量高,着色强烈,使这些化合物适用于染料。
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引用次数: 5
Design, synthesis and anti-bacterial evaluation of novel 1,3,4-thiadiazole derivatives bearing a semicarbazone moiety 新型含氨基脲类1,3,4-噻二唑衍生物的设计、合成及抗菌评价
Pub Date : 2018-02-26 DOI: 10.1080/10426507.2018.1436546
Jin-Lin Wan, Yiyuan Gan, Wei-nan Hu, Jiao Meng, Kun Tian, Xiao-qin Li, Shou-Qun Wu, Yang Xu, Gui-ping Ouyang, Zhenchao Wang
GRAPHICAL ABSTRACT ABSTRACT Novel 1,3,4-thiadiazole derivatives bearing a semicarbazone moiety were prepared and evaluated for their anti-bacterial activities against Xanthomonas oryzae pv. oryzae (Xoo) and Xanthomonas axonopodis pv. citri (Xac) by performing a turbidimetre test. The products were structurally characterised by IR, 1H NMR, 13C NMR, 19F NMR and HRMS. Anti-bacterial testing showed that most of the evaluated compounds (6a-6s) exhibited excellent activity (≥74.19%) against Xoo at a concentration of 200 µg/mL, with 50% effective concentration (EC50) values ranging from 12.21 to 67.20 µg/mL, which were superior to the commercial antibacterial agent bismerthiazol (92.23 µg/mL). Among them, compound 2-((2-chloro-1H-indol-3-yl)methylene)-N-(5-((2-chlorobenzyl)thio)-1,3,4-thiadiazol-2-yl)hydrazine-1-carboxamide (6b) demonstrated good inhibitory activity against Xac (89.46% at 200 µg/mL) and Xoo (EC50 = 18.28 µg/mL); compound 2-((2-chloro-1H-indol-3-yl)methylene)-N-(5-((4-methoxybenzyl)thio)-1,3,4-thiadiazol-2-yl)hydrazine-1-carboxamide (6g) displayed excellent activity against Xoo with EC50 value of 12.21 µg/mL.
摘要本文制备了含有缩氨基脲基团的新型1,3,4-噻二唑衍生物,并对其抑菌活性进行了评价。稻瘟病菌(Xoo)和轴尾黄单胞菌(Xanthomonas axonopodis pv)。柠檬酸(Xac)进行浊度计试验。通过IR、1H NMR、13C NMR、19F NMR和HRMS对产物进行了结构表征。抑菌试验结果表明,大部分化合物(6a-6s)在200µg/mL的浓度下对Xoo具有良好的抑菌活性(≥74.19%),50%有效浓度(EC50)在12.21 ~ 67.20µg/mL之间,优于市售抗菌剂双硫噻唑(92.23µg/mL)。其中,化合物2-((2-氯- 1h -吲哚-3-基)亚甲基)- n -(5-(2-氯苯基)硫)-1,3,4-噻二唑-2-基)肼-1-羧酰胺(6b)对Xac和Xoo具有良好的抑制活性(200µg/mL时为89.46%)(EC50 = 18.28µg/mL);化合物2-((2-氯- 1h -吲哚-3-基)亚甲基)- n -(5-(4-甲氧基苄基)硫)-1,3,4-噻二唑-2-基)肼-1-羧酰胺(6g)对Xoo具有良好的抑菌活性,EC50值为12.21µg/mL。
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引用次数: 4
Three-component reaction for an efficient synthesis of 5-hydroxy-1-phenyl-1H-pyrazoles containing a stable phosphorus ylide moiety 三组分反应高效合成含稳定磷酰化基团的5-羟基-1-苯基- 1h -吡唑
Pub Date : 2018-02-23 DOI: 10.1080/10426507.2018.1437619
Ehsan Ghonchepour, M. Islami, H. Mostafavi, Ahmad Momeni Tikdari
GRAPHICAL ABSTRACT ABSTRACT A concise synthesis of new polysubstituted pyrazoles containing a phosphorane is achieved from readily available organic compounds. This C–H bond functionalization is an efficient means of selectively substituting 4-position of pyrazole to produce a five-membered aromatic ring with a chain containing ylide moiety. This protocol requires no additional catalyst and can be used for other pyrazoles including different substituents.
摘要:本文以易得的有机化合物为原料,合成了一种含磷烷的新型多取代吡唑。这种C-H键功能化是一种选择性取代吡唑4位的有效方法,它可以生成含有乙烯基的五元芳香环。该方法不需要额外的催化剂,可用于包括不同取代基的其他吡唑。
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引用次数: 8
Expeditious synthesis of 9-allenylpurines via cesium carbonate catalyzed isomerization of 9-alkynylpurines 碳酸铯催化9-炔基嘌呤异构化快速合成9-烯基嘌呤
Pub Date : 2018-02-13 DOI: 10.1080/10426507.2018.1436547
Mingwu Yu, Xiguang Liu, Q. Jiang, H. Du
GRAPHICAL ABSTRACT ABSTRACT An expeditious and convenient method to synthesize 9-allenylpurines via cesium carbonate catalyzed isomerization of 9-alkynylpurines has been successfully developed. The reactions proceeded rapidly under the base conditions and formed the desired products in good to excellent yields. The method was suitable with a broad substrate scope and proceeded well even on a multgram-scale. The obtained 9-allenylpurines were successfully applied to prepare various potential bioactive 9-acyclic nucleosides with high regioselectivity promoted by AgNO3.
摘要建立了一种快速、简便的碳酸铯催化9-炔基嘌呤异构化合成9-烯基嘌呤的方法。该反应在碱条件下进行迅速,并以优异的收率生成所需的产物。该方法适用于广泛的衬底范围,即使在多克尺度上也能很好地进行。得到的9-烯基嘌呤被成功地应用于制备多种具有高区域选择性的具有潜在生物活性的9-无环核苷。
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引用次数: 2
Ag+-ion implantation of silicon 银离子注入硅
Pub Date : 2018-02-01 DOI: 10.1080/10426507.2017.1417307
A. Stepanov, V. Nuzhdin, V. Valeev, V. Vorobev, Y. Osin
GRAPHICAL ABSTRACT ABSTRACT The new results on the optical reflection of the Si surface layers implanted by silver ions at low energies of 30 keV over a wide dose range from 5.0 × 1014 to 1.5 × 1017 ion/cm2 are presented. As the ion dose of irradiation was increased, a monotonic decrease in the reflection intensity in the ultraviolet region of the spectrum was observed, due to amorphization and macrostructuring of the Si surface. On the other hand, in the long-wavelength region, a selective reflection band appears with a maximum near 830 nm due to plasmon resonance of Ag nanoparticles synthesized during implantation.
摘要本文给出了低能量30 keV的银离子在5.0 × 1014 ~ 1.5 × 1017离子/cm2宽剂量范围内注入硅表面层的光学反射的新结果。随着离子辐照剂量的增加,由于Si表面的非晶化和宏观结构,光谱紫外区的反射强度单调下降。另一方面,在长波长区域,由于植入过程中合成的银纳米粒子的等离子体共振,在830 nm附近出现了一个选择性反射带,最大反射带在830 nm附近。
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引用次数: 1
An algorithm for boron diffusion in MOS transistors using Silvaco Athena and MATLAB 基于Silvaco Athena和MATLAB的MOS晶体管硼扩散算法
Pub Date : 2018-02-01 DOI: 10.1080/10426507.2017.1417305
N. Guenifi, R. Mahamdi, I. Rahmani
GRAPHICAL ABSTRACT ABSTRACT In this paper we have developed an algorithm of boron diffusion after thermal annealing in a highly doped polysilicon film. This algorithm takes into account electrically active point defects by associating some parameters such as boron solubility limit and diffusion coefficient. We have studied effect of annealing temperature in order to perform impact of this parameter on maximum depth diffusion of junction and maximum of concentration by analysis of Secondary Ion Mass Spectrometry (SIMS) profiles. In fact we have proposed numerical model based on Fick's equation, resolved by finite difference method under Matlab also we have simulated this phenomenon by Silvaco software.
摘要本文提出了一种在高掺杂多晶硅薄膜中热退火后硼扩散的算法。该算法结合硼溶解度极限和扩散系数等参数,考虑了电活性点缺陷。通过二次离子质谱(SIMS)分析,研究了退火温度对结最大扩散深度和最大扩散浓度的影响。事实上,我们已经提出了基于Fick方程的数值模型,在Matlab下用有限差分法求解,并利用Silvaco软件对这一现象进行了模拟。
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引用次数: 1
Co-assembled ZnO (shell) – CuO (core) nano-oxide materials for microbial protection 协同组装ZnO(壳)- CuO(芯)纳米氧化物材料用于微生物保护
Pub Date : 2018-02-01 DOI: 10.1080/10426507.2017.1417301
K. Varaprasad
GRAPHICAL ABSTRACT ABSTRACT Development of efficient antimicrobial metal-oxide nanoparticles (MONPs) is important to advance in the biomedical and in the industrial fields. Herein, ZnO-CuO nanoparticles with improved antibacterial were developed by simple double precipitation technique and their properties were studied. The bactericide ability of ZnO-CuO nanoparticles was investigated against Escherichia coli. The ZnO-CuO0.5 exhibited high activity against E.coli at high and low concentration levels. The MONPs were analyzed via FTIR, UV-visible/DRS, PL, SEM/EDS, TEM, XRD and TGA analysis. These results show the formation of hexagonal wurtzite-monoclinic phase morphology and the thermal characteristics of the ZnO-CuO nanoparticles emphasize the potential of these dual nanooxide materials. The intensity of the emission band of ZnO was decreased following the increase in the CuO concentrations and the order is as follows: CuO < ZnO-CuO0.5 < ZnO-CuO0.1 < ZnO. The co-assembled MONPs developed may function as potential candidates for advanced biomedical and industrial applications.
摘要高效抗菌金属氧化物纳米颗粒(MONPs)的开发对生物医学和工业领域的发展具有重要意义。本文采用简单双沉淀法制备了具有增强抗菌性能的ZnO-CuO纳米颗粒,并对其性能进行了研究。研究了ZnO-CuO纳米颗粒对大肠杆菌的杀菌能力。ZnO-CuO0.5在高、低浓度下均表现出较高的抑菌活性。通过FTIR, UV-visible/DRS, PL, SEM/EDS, TEM, XRD和TGA分析对MONPs进行了分析。这些结果表明,六方纤锌矿-单斜相形态的形成和ZnO-CuO纳米颗粒的热特性强调了这些双纳米氧化物材料的潜力。ZnO的发射带强度随CuO浓度的增加而减小,其顺序为:CuO < ZnO- cuo0.5 < ZnO- cuo0.1 < ZnO。所开发的共组装MONPs可作为先进生物医学和工业应用的潜在候选者。
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引用次数: 11
Focalizing slow neutron beams at and below micron scales: Discussion on BNCT 微米及微米以下的慢中子束聚焦:关于BNCT的讨论
Pub Date : 2018-02-01 DOI: 10.1080/10426507.2017.1417300
R. F. Álvarez-Estrada, I. M. de la Peña, M. L. Calvo
GRAPHICAL ABSTRACT ABSTRACT We outline some general properties of slow neutrons and their interactions in material media, their use in Boron Neutron Capture Therapy (BNCT) and their waveguiding properties. We review two important experiments on slow neutron confined propagation: in thin films and in polycapillary glass fibres. Based upon the first experiment and on previous proposals, we formulate two new proposals regarding possibilities for improved focalization (at and a bit below one micron) and propagation along longer lengths (up to about 1 m) with relatively small attenuation, and discuss possible implications for BNCT of small tumours. We emphasize the general interest and possible applications of exploring short scales by means of slow neutrons, through suitable combinations of the devices involved in those two experiments.
摘要本文概述了慢中子的一些一般性质及其在材料介质中的相互作用、慢中子在硼中子俘获治疗(BNCT)中的应用以及慢中子的波导性质。本文综述了两个关于慢中子在薄膜和多毛细玻璃纤维中受限传播的重要实验。基于第一个实验和先前的建议,我们提出了两个关于改进聚焦(在1微米和略低于1微米)和沿较长长度(高达约1米)传播的可能性的新建议,衰减相对较小,并讨论了对小肿瘤BNCT的可能影响。我们强调通过这两个实验中所涉及的设备的适当组合,利用慢中子探索短尺度的普遍兴趣和可能的应用。
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引用次数: 4
Characterizing slow state near Si-SiO2 in MOS structure MOS结构中近Si-SiO2慢态的表征
Pub Date : 2018-02-01 DOI: 10.1080/10426507.2017.1417303
N. Guenifi, D. Bauza, R. Mahamdi
GRAPHICAL ABSTRACT ABSTRACT The Equilibrium Voltage Step (EVS) technique has been used for extraction of depth and energy concentration profile of traps situated in the oxide of a lightly stressed metal-oxide-semiconductor (MOS) structure. This has been achieved up to the very near Si-SiO2 interface. The results are discussed and compared with those obtained using charge pumping (CP) technique. A good agreement is achieved between the trap densities extracted using the two methods even though differences in the shape of the profiles can be observed. The results also very well agree with those published previously using current deep level transient spectroscopy (C-DLTS).
摘要平衡电压阶跃(EVS)技术用于提取位于轻应力金属-氧化物-半导体(MOS)结构氧化物中的陷阱的深度和能量浓度分布。这已经达到了非常接近Si-SiO2界面。讨论了所得结果,并与电荷泵送(CP)技术所得结果进行了比较。尽管可以观察到剖面形状的差异,但使用两种方法提取的陷阱密度之间取得了很好的一致性。结果也与先前发表的使用当前深能级瞬态光谱(c - dlt)的结果非常一致。
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引用次数: 1
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Phosphorus Sulfur and Silicon and The Related Elements
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