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Synthesis of 5-substituted-1,3,4-oxadiazole clubbed pyrazole and dihydropyrimidine derivatives as potent bioactive agents 5-取代-1,3,4-恶二唑棒状吡唑及二氢嘧啶衍生物的合成
Q3 Chemistry Pub Date : 2021-01-01 DOI: 10.17628/ecb.2021.10.13-20
B. Patel, Tushar J. Karkar, Malay J. Bhatt
A series of 4-fluorophenylpyrazole clubbed 1,3,4-oxadiazole and 3,4-dihydropyrimidin-2(1 H )-ones were prepared by cyclization of Biginelli-type adducts. Structures were assigned on the basis of known spectral techniques. All the scaffolds were evaluated for in vitro antimicrobial activity by broth micro dilution bioassay method and in vitro antitubercular property by microplate alamar blue assay method. Compounds 3j and 3l containing -OH and -CH 3 groups were act as potent antimicrobials and antitubercular candidates with relatively low cytotoxicity on VERO cells.
以biginelli型加合物为环,制备了一系列含1,3,4-恶二唑和3,4-二氢嘧啶-2(1 H)-的4-氟苯吡唑。结构是根据已知的光谱技术分配的。采用微量肉汤稀释法测定支架的体外抗菌活性,用微孔板阿拉马尔蓝法测定支架的体外抗结核性能。含有-OH和-CH - 3基团的化合物3j和3l对VERO细胞具有较低的细胞毒性,是有效的抗菌剂和抗结核候选药物。
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引用次数: 7
Synthesis of novel anti-inflammatory usnic acid-based imidazolium salts 新型抗炎酸基咪唑盐的合成
Q3 Chemistry Pub Date : 2021-01-01 DOI: 10.17628/ecb.2021.10.67-72
T. Somasekhar, Monisha Javadi, R. Sistla, U. Mallavadhani
Ten novel usnic acid based imidazolium salts were synthesized by employing a two-step protocol. The anti-inflammatory potential of the newly synthesised compounds was evaluated in vitro against cytokine proteins TNF- α and IL - 1 β secreted from U937 cells. Some of the imidazolium salts exhibited promising anti-inflammatory activity against the TNF- α and IL - 1β with IC 50 values ranging between 5.3 μM - 7.5 μM, which are many folds lower than that of the parent compound (>100 μM). Most significantly, substitution with electronegative groups in imidazolium salts of usnic acid found to be more potent and exhibiting enhanced anti-inflammatory activity.
采用两步法合成了10种新型的usic酸基咪唑盐。新合成的化合物在体外对U937细胞分泌的细胞因子蛋白TNF- α和IL - 1 β的抗炎潜力进行了评估。部分咪唑盐对TNF- α和IL - 1β具有良好的抗炎活性,其IC 50值在5.3 μM ~ 7.5 μM之间,比母体化合物(> ~ 100 μM)低许多倍。最重要的是,在咪唑盐中与电负性基团的取代被发现更有效,并表现出增强的抗炎活性。
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引用次数: 1
Synthesis, characterization and antimicrobial activity of transition metal complexes of 4-[(2-hydroxy-4-methoxyphenyl)methyleneamino]-2,4-dihydro-3H-1,2,4-triazole-3-thione 4-[(2-羟基-4-甲氧基苯基)亚甲基氨基]-2,4-二氢-3H-1,2,4-三唑-3-硫酮过渡金属配合物的合成、表征及抗菌活性
Q3 Chemistry Pub Date : 2020-12-13 DOI: 10.17628/ecb.2020.9.430-435
S. P. Bhale, A. Yadav, Pintu G. Pathare, S. Tekale, F. P. Franguelli, L. Kótai, R. Pawar
A novel nitrogen containing 4-[(2-hydroxy-4-methoxyphenyl)methyleneamino]-2,4-dihydro-3H-1,2,4-triazole-3-thione ligand (H2L) was synthesized by using an equimolar ratio of 4-amino-1,2,4-triazole-3-thione and 2-hydroxy-4-methoxybenzaldehyde. A series of Mn(II), Co(II), Ni(II), Cu(II), Zn(II) and Cd(II) complexes was synthesized by using the ligand. The synthesized ligand and transition metal complexes were characterized by IR, 1H NMR, 13C NMR, Mass spectrometry, UV, XRD and TGA investigation methods. Spectral data suggests that the ligand acts as a tridentate SNO donor. Further, the synthesized H2L ligand and their metal complexes were screened for antimicrobial activity. The results of biological activities showed that the metal complexes have higher antifungal as well as antibacterial activity as compared to the parent H2L ligand against the tested microbes.
以4-氨基-1,2,4-三唑-3-硫酮和2-羟基-4-甲氧基苯甲醛等摩尔比合成了一种新型含氮4-[(2-羟基-4-甲氧基苯基)亚甲基氨基]-2,4-二氢-3H-1,2,4-三唑-3-硫代酮配体(H2L)。利用该配体合成了一系列Mn(II)、Co(II),Ni(II)和Cu(II)以及Zn(II)与Cd(II)的配合物。用红外光谱、核磁共振氢谱、核磁共振13C谱、质谱、紫外光谱、X射线衍射和热重分析等方法对合成的配体和过渡金属配合物进行了表征。光谱数据表明,配体起到了三齿SNO供体的作用。此外,对合成的H2L配体及其金属配合物进行了抗菌活性筛选。生物活性的结果表明,与母体H2L配体相比,金属配合物具有更高的抗真菌和抗菌活性。
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引用次数: 4
Leaves peroxidase and esterase isozymes in sunflower crops exposed to saline environment 盐渍环境下向日葵叶片过氧化物酶和酯酶同工酶的研究
Q3 Chemistry Pub Date : 2020-12-05 DOI: 10.17628/ecb.2020.9.425-429
Chadia Ouazzani, A. Moustaghfir, A. Er-Ramly
Water deficit stress is one of the main problems determining the yield of many crop plants. The study of the effects of salinity on plant growth and development and the search for biochemical stress markers are of great importance in the selection of resistant species. Accumulation and antioxidant activities in response to salinity at different sunflower varieties constitute markers for genetic selection and improvement of plants in the face of tolerance to salinity. Electrophoretic analysis of zymograms of different sunflower varieties grown in a saline environment for 40 days revealed zymograms of peroxidases and esterases specific to varieties tolerant to the saline environment. Peroxidases activity extracted from leaves is augmented in relation to their involvement in the physiological process related to salinity tolerance. In susceptible varieties, peroxidases activity is decreased compared to normal conditions. Variability of activity and polymorphism of isozyme peroxidases and esterases in response to salinity at different sunflower varieties constitute markers for genetic selection and plant improvement in the face of salinity tolerance.
水分亏缺胁迫是决定许多作物产量的主要问题之一。研究盐度对植物生长发育的影响,寻找生化胁迫标记,对抗性品种的选择具有重要意义。不同向日葵品种对盐胁迫的积累和抗氧化活性是植物耐盐性遗传选择和改良的标志。对不同向日葵品种在盐渍环境中生长40 d的酶谱进行电泳分析,发现耐盐渍向日葵品种的过氧化物酶和酯酶谱具有特异性。从叶片中提取的过氧化物酶活性增强与其参与与耐盐性相关的生理过程有关。在敏感品种中,过氧化物酶活性比正常条件下降低。不同向日葵品种同工酶过氧化物酶和酯酶对盐胁迫的活性变异和多态性为耐盐遗传选择和植物改良提供了依据。
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引用次数: 0
Synthesis of acetins from ethyl acetate via transesterification with glycerol using a sulphonic acid type ion-exchange resin 磺酸型离子交换树脂与甘油酯交换合成乙酸乙酯
Q3 Chemistry Pub Date : 2020-11-29 DOI: 10.17628/ecb.2020.9.420-424
Sravanthi Veluturla, Archna Narula, Kamolpun Sathitsommon, L. V. Anirudh
Demand for biodiesel has increased over the years as a substitute to petrol and diesel due to its environmental-friendly nature and lower cost. Glycerol being major by-product of the process constitutes 10 wt.% of the products hence conversion of glycerol to value added products such as acetins in the plant reduces the production cost of biodiesel. The present work focuses on the transesterification reaction between glycerol and ethyl acetate over heterogeneous catalyst, Amberlyst-15(wet). The batch studies were carried out and the effect of reaction parameters such as reaction time (1-7 h), glycerol to ethyl acetate molar ratio (1:3-1:12), temperature (50-70 o C), catalyst loading (2-5 w/w%) have been studied. The maximum conversion of glycerol obtained at (G : EA) molar ratio 1:6, reaction temperature of 70 ˚C and 4 w/w% catalyst loading for 7 h was 97.71 % and the selectivity of mono-, di- and triacetins were 36.7, 60.7 and 2.51 %, respectively. This provides an eco-friendly and sustainable path for valorisation of biodiesel derived glycerol.
近年来,生物柴油作为汽油和柴油的替代品,由于其环保和成本较低,对其的需求有所增加。甘油是该过程的主要副产品,占产品的10%,因此在工厂中将甘油转化为附加值产品,如乙酰,降低了生物柴油的生产成本。本研究的重点是甘油和乙酸乙酯在非均相催化剂Amberlyst-15(湿)上的酯交换反应。对反应时间(1 ~ 7 h)、甘油与乙酸乙酯的摩尔比(1:3 ~ 1:12)、温度(50 ~ 70℃)、催化剂负载(2 ~ 5 w/w%)等参数的影响进行了批量研究。在(G: EA)摩尔比为1:6、反应温度为70℃、催化剂负载为4 w/w%、反应时间为7 h的条件下,甘油的最大转化率为97.71%,单乙酰、二乙酰和三乙酰的选择性分别为36.7%、60.7%和2.51%。这为生物柴油衍生甘油的增值提供了一个生态友好和可持续的途径。
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引用次数: 1
Stabilization of dioxochromium(VI) in the complex with tetra[benzo]porphyrazine and two oxo ligands: DFT quantum-chemical consideration 四[苯并]卟啉和两个氧配体配合物中二氧铬(VI)的稳定性:DFT量子化学的考虑
Q3 Chemistry Pub Date : 2020-11-25 DOI: 10.17628/ecb.2020.9.416-419
O. Mikhailov, D. Chachkov
Based on the results of a quantum chemical consideration in the framework of DFT OPBE/TZVP and B3PW91/TZVP methods, the possibility of the self-existence of a chromium heteroligand complex with (NNNN)-donor macrocyclic ligand – tetra[benzo]porphyrazine and two oxo ligands where chromium oxidation degree is (+6), have been shown. The data on the key structural parameters and also, on multiplicity of the ground state of the given macrocyclic metal complex have also been presented.
基于DFT OPBE/TZVP和B3PW91/TZVP方法框架下的量子化学考虑结果,显示了铬与(NNNN)-供体大环配体-四[苯并]卟啉和两个氧代配体的杂铬配体络合物自身存在的可能性,其中铬氧化度为(+6)。给出了大环金属配合物的关键结构参数和基态多重性的数据。
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引用次数: 4
Synthesis, molecular docking and anti-inflammatory activity 2,4-dimethyl-N-(2-aryl)-3-furamides 2,4-二甲基-N-(2-芳基)-3-呋喃酰胺的合成、分子对接及抗炎活性
Q3 Chemistry Pub Date : 2020-11-22 DOI: 10.17628/ecb.2020.9.410-415
Y. Matiichuk, Y. Horak, T. Chaban, V. Ogurtsov, L. Kostyshyn, V. Matiychuk
2,4-Dimethyl-N-aryl-3-furamides were synthesized by the reaction of 2,4-dimethyl-furan-3-carbonyl chloride with aromatic amines in dry dioxane in the presence of triethylamine. The structures of the obtained substances were confirmed by 1H NMR spectroscopy and elemental analysis. The synthesized compounds were preselected via molecular docking to be tested for their anti-inflammatory activity. The anti-inflammatory effect of the prepared compounds was investigated applying the carrageenan-induced paw edema model. The results have shown that the some novel furamides demonstrated considerable anti-inflammatory effect.
以2,4-二甲基呋喃-3-羰基氯为原料,在三乙胺存在下,在干二恶烷中与芳香胺反应合成2,4-二甲基- n-芳基-3-呋喃酰胺。所得物质的结构经核磁共振氢谱和元素分析证实。通过分子对接预先选择合成的化合物,测试其抗炎活性。采用角叉菜胶致足跖水肿模型,研究所制化合物的抗炎作用。结果表明,一些新型呋喃酰胺具有明显的抗炎作用。
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引用次数: 0
Synthesis, thermal stability and kinetic studies of copper(II) and cobalt(II) complexes derived from 4-aminobenzohydrazide and 2-mercaptobenzothiazole 4-氨基苯甲酰肼和2-巯基苯并噻唑铜(II)和钴(II)配合物的合成、热稳定性和动力学研究
Q3 Chemistry Pub Date : 2020-11-11 DOI: 10.17628/ecb.2020.9.403-409
Maged S. Al-Fakeh
The divalent transition metal ions Cu (II) and Co (II) compounds of the formula; [ M(ABZH)(MBTH)Cl 2 (H 2 O) 2 ], (M = Cu (II) and Co (ІІ), ABZH=4-Aminobenzohydrazide (L1) and MBTH = 2-mercaptobenzthiazole (L2) have been synthesized and characterized. The two compounds has been designated based on elemental analysis, electronic spectral analysis, FT-IR , magnetic measurements and XRD. The thermal properties of copper(II) and cobalt(II) metal compounds in dynamic air have been analyzed via thermogravimetry(TG), and differential thermogravimetry(DTG). The kinetic analyses of the thermal decomposition for the two compounds were calculated by the Coats.Redfern and Horowitz.Metzger methods. The obtained kinetic parameters, display the kinetic compensation effect(KCE).
式的二价过渡金属离子Cu(II)和Co(II)化合物;合成并表征了[M(ABZH)(MBTH)Cl2(H2 O)2],(M=Cu(II)和Co(?),ABZH=4-氨基苯并酰肼(L1)和MBTH=2-巯基苯并噻唑(L2)。根据元素分析、电子光谱分析、FT-IR、磁性测量和XRD对这两种化合物进行了表征。通过热重分析(TG)和差热分析(DTG)对铜(II)和钴(II)金属化合物在动态空气中的热性能进行了分析。通过Coats计算了两种化合物的热分解动力学分析。雷德芬和霍洛维茨。Metzger方法。获得的动力学参数显示了动力学补偿效应(KCE)。
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引用次数: 6
Development of promising cathode materials based on modified spinels for Li-Ion batteries 基于改性尖晶石的锂离子电池正极材料研究进展
Q3 Chemistry Pub Date : 2020-11-04 DOI: 10.17628/ecb.2020.9.401-402
E. Kachibaia, T. Paikidze, R. Imnadze, Shukri S. Japaridze
Lithium rich compounds represent a promising cathode material of Li-ion accumulators due to their valuable electrochemical properties and represent cathode material of the next generation high-performance lithium-ion batteries.2,3 These compounds are of great interest mostly because of the high capacity exceeding 250 mAh g-1. However, a number of disadvantages, such as voltage drop caused by unwanted phase transformations during cycling, as well as low operational performances still limit their application. Improved cycling stability can be achieved by cathode materials doping (modification). Regarding costs and raw materials, Fe-Mn-based systems are economically attractive cathodes for LIB containing Fe as a cheap promising alternative to commercial LiCoO2 and LiMn2O4.
富锂化合物由于其宝贵的电化学性能,是锂离子蓄电池的一种很有前途的正极材料,也是下一代高性能锂离子电池的正极材料。2,3这些化合物之所以备受关注,主要是因为其高容量超过250 mAh g-1。然而,许多缺点,例如在循环过程中由不希望的相变引起的电压降,以及低的操作性能仍然限制了它们的应用。阴极材料的掺杂(改性)可以提高循环稳定性。关于成本和原材料,Fe-Mn基系统是含有Fe的LIB的经济上有吸引力的阴极,是商业LiCoO2和LiMn2O4的廉价、有前途的替代品。
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引用次数: 1
Amaranthaceae plants of Israel and Palestine: Medicinal activities and unique compounds 以色列和巴勒斯坦苋科植物:药用活性和独特化合物
Q3 Chemistry Pub Date : 2020-10-31 DOI: 10.17628/ecb.2020.9.366-400
A. Azab
Amaranthaceae family is one of the largest and most diverse in the plant kingdom. While some of the plants of this family have important nutritional value, others are considered toxic and/or hazardous weeds and many efforts have been made in controlling them. But both categories were used by humans for traditional medicinal purposes, and some of them were extensively studied by modern science. In this review article, we will present some ethnomedicinal uses of the plants of this family, along with comprehensive literature survey of medicinal, biological and other activities. Information will be presented in tables for the convenience of readers, and many structures of natural products are presented. The extensive discussion section will focus mainly (but not only) on studies of active compounds production. This review article is about plants of this family in general and in particular about Amaranthaceae plants of our region. Conclusions and future research recommendations are also presented.
苋科是植物王国中最大和最多样化的植物之一。虽然这一科的一些植物具有重要的营养价值,但其他植物被认为是有毒和/或有害的杂草,人们已经做出了许多努力来控制它们。但这两种类型都被人类用于传统的医学目的,其中一些被现代科学广泛研究。本文将介绍该科植物的一些民族医学用途,并对其药用、生物学和其他方面的药理作用进行文献综述。为了方便读者,信息将以表格的形式呈现,并展示了许多天然产物的结构。广泛的讨论部分将主要关注(但不仅限于)活性化合物生产的研究。本文综述了苋科植物的概况,重点介绍了我国苋科植物的生长情况。最后提出结论和未来的研究建议。
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引用次数: 0
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European Chemical Bulletin
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