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Π-Extended Systems Based on Tetracyclic Benzo [4,5] Imidazo [2′,1′:6,1] Pyrido[2,3-D] Pyrimidines Π-Extended基于四环苯并[4,5]咪唑[2 ',1 ':6,1]吡啶[2,3- d]嘧啶的体系
Pub Date : 2019-04-08 DOI: 10.19080/omcij.2019.08.555737
Harutyunyan Artur A
Recently, we have developed a fundamentally new method of constructing the derivatives of the heterocyclic system of benzo[4′,5] imidazo[2′,1′:6,1]pyrido[2,3-d]pyrimidine [1], which allowed the introduction of methyl and methylene into the molecule groups. It should be noted that some derivatives of the indicated heterocyclic system revealed antibacterial and ant monoamine oxidase properties [2,3].
最近,我们开发了一种全新的方法来构建苯并[4 ',5]咪唑[2 ',1 ':6,1]吡啶[2,3-d]嘧啶[1]杂环体系的衍生物,这种方法允许在分子基中引入甲基和亚甲基。值得注意的是,该杂环体系的一些衍生物显示出抗菌和抗单胺氧化酶的特性[2,3]。
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引用次数: 0
Green Synthesis, Spectral, Thermal Characterization and Biological Activity of Schiff base Ligand Derived from 3-amino-1,2,4-triazol and its Metal Complexes 3-氨基-1,2,4-三唑及其金属配合物希夫碱配体的绿色合成、光谱、热表征及生物活性
Pub Date : 2019-03-14 DOI: 10.19080/omcij.2019.08.555736
A. Mm
Green, efficient and clean synthesis of a Schiff base ligand, 1-(((1H-1,2,4-triazol-3-yl) imino) methyl) naphthalen-2-ol (TMN) has been synthesized in equimolar reaction (1:1) of 3-amino-1,2,4-triazole as a primary amine and 2-hydroxy-1-naphthaldehyde as an aldehyde using microwave irradiation technique. The synthesized Schiff base ligand was then reacted with four transition metal ions Co(II), Ni(II), Cu(II) and Zn(II) in 1:1 molar ratio of ligand and metal acetate using microwave technique. The stereochemistry and the bonding characteristics of the ligand and its metal complexes were achieved based on elemental analysis, FT-IR, UV-Vis., NMR and ESR as well as Thermo-Gravimetric Analysis (TGA). The thermal dehydration and decomposition of Co (II), Ni(II) and Cu(II) complexes were studied kinetically using the integral method applying the Coats-Redfern and Horowitz Metzger equations. The antimicrobial activities of ligand and its Zn (II) complex were studied against the bacterial (positive and negative) grams and
采用微波辐照技术,以3-氨基-1,2,4-三唑为伯胺,2 -羟基-1-萘醛为醛,以1:1的等摩尔反应合成了希夫碱配体1-(((1h -1,2,4-三唑-3-基)亚氨基)甲基)萘-2-醇(TMN)。将合成的席夫碱配体与四个过渡金属离子Co(II)、Ni(II)、Cu(II)和Zn(II)以配体与金属醋酸酯1:1的摩尔比进行微波反应。通过元素分析、红外光谱(FT-IR)、紫外-可见光谱(UV-Vis)表征了配体及其金属配合物的立体化学和成键特性。核磁共振和ESR以及热重分析(TGA)。采用Coats-Redfern方程和Horowitz Metzger方程,采用积分法研究了Co (II)、Ni(II)和Cu(II)配合物的热脱水分解动力学。研究了配体及其Zn (II)配合物对细菌(正、负)克和细菌的抑菌活性
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引用次数: 4
Design and Synthesis of Antifungal Compounds from 1,2,3-Triazoles through the Click Chemistry Approach 1,2,3-三唑类抗真菌化合物的设计与合成
Pub Date : 2019-03-12 DOI: 10.19080/omcij.2019.08.555734
Erick Cuevas Yañez
1,2,3-triazoles are easily prepared from CuAAC reaction and represent a potential source of antifungal compounds analogous to azole drugs. Accordingly, research groups have synthesized diverse 1,2,3-triazoles with modulated antifungal activity through the substituents in azide or alkyne precursors. A brief review of the state of the art about this topic is presented, focusing the increasing importance of developing new and more selective antifungal compounds.
1,2,3-三氮唑是一种很容易由CuAAC反应制备的抗真菌化合物,是一种类似于唑类药物的潜在来源。因此,研究小组通过叠氮或炔前体中的取代基合成了多种具有调节抗真菌活性的1,2,3-三唑。简要回顾了有关这一主题的最新进展,重点介绍了开发新的和更具选择性的抗真菌化合物的重要性。
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引用次数: 2
A Mini Review of Catalytic Reducing Nitrogen to Ammonia under Ambient Conditions 环境条件下催化还原氮制氨技术综述
Pub Date : 2019-02-26 DOI: 10.19080/omcij.2019.08.555732
Jian-Jhe Yang
Ammonia(NH 3 ) has played an essential role in meeting the increasing demand for food and the worldwide need of nitrogenous fertilizer since 1913. Unfortunately, the traditional Haber-Bosch process for producing NH 3 from nitrogen(N 2 ) is a high energy-consumption process. Under ambient conditions catalytic reducing N 2 to NH 3 is an attractive and promising alternative approach which would emerge huge opportunity to directly provide nitrogenous fertilizers in agricultural fields as need in a distributed manner. In this review, some research findings showed alterna -tive, available, sustainable NH 3 production processes from N 2 in the presence of electro-catalysts and photo-catalysts under ambient conditions.
自1913年以来,氨(nh3)在满足日益增长的粮食需求和全球氮肥需求方面发挥了重要作用。不幸的是,从氮(n2)中生产nh3的传统Haber-Bosch工艺是一个高能耗的过程。在环境条件下,催化还原n2为nh3是一种极具吸引力和前景的替代方法,它将为农业领域直接按需分布式提供氮肥提供巨大的机会。在此综述中,一些研究结果表明,在电催化剂和光催化剂的存在下,在环境条件下,n2可替代、可用、可持续地生产nh3。
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引用次数: 0
Spectroscopic and Calorimetric Evaluation of the Biofield Energy Healing Treated Ofloxacin 氧氟沙星生物场能量愈合的光谱和量热评价
Pub Date : 2019-02-21 DOI: 10.19080/OMCIJ.2019.08.555731
G. Nayak, M. Trivedi, A. Branton, Dahryn Trivedi, S. Jana
Ofloxacin is an antibiotic useful for the treatment of bacterial infections. The aim of this research work was to evaluate the impact of the Trivedi Effect®-Consciousness Energy Healing Treatment on the physicochemical properties of ofloxacin using modern analytical techniques. The sample was divided into control and Biofield Energy Treated parts. The control sample did not receive the Biofield Energy Treatment; whereas, the treated part received the Biofield Treatment remotely by a famous Biofield Energy Healer, Gopal Nayak. The PXRD peak intensities and crys-tallite sizes were significantly altered ranging from -39.33% to 127.93% and -68.28% to 21%, respectively; however, the average crystallite size of the treated ofloxacin (236.59nm) was decreased by 19.48% compared with the control sample (293.83nm). The particle size values were signifi-cantly decreased at d10 (10.67%), d50 (25%), d90 (24.4%), and D (4,3) (25.12%); thus, the specific surface area was significantly increased by 9.8% in the treated sample compared to the control sample. The latent heat of fusion and the latent heat of decomposition of the treated sample were significantly increased by 11.71% and 123.52%, respectively compared to the control sample. The total weight loss was significantly decreased by 10.59%; however, the residue amount was significantly increased by 63.29% in the treated ofloxacin compared with the control sample. The Trivedi Effect®-Consciousness Energy Healing Treatment generated a new polymorphic form of ofloxacin which may be more soluble, bioavail-able, and be thermally more stable compared to the untreated sample. The treated ofloxacin would be more efficacious against cellulitis, prosta-titis, chronic bronchitis, urinary tract infections, infections of the urethra and cervix, pneumonia, infectious diarrhoea, plague, etc.
氧氟沙星是一种用于治疗细菌感染的抗生素。本研究的目的是利用现代分析技术评估Trivedi效应®-意识能量治疗对氧氟沙星理化性质的影响。样品分为对照部分和生物场能量处理部分。对照样品未接受生物场能量处理;而被治疗的部分则由著名的生物场能量治疗师Gopal Nayak远程进行生物场治疗。PXRD峰强度和结晶高粒石尺寸变化明显,分别为-39.33% ~ 127.93%和-68.28% ~ 21%;但处理后的氧氟沙星的平均晶粒尺寸(236.59nm)比对照样品(293.83nm)减小了19.48%。d10(10.67%)、d50(25%)、d90(24.4%)和D(4,3)(25.12%)的粒径值显著降低;因此,与对照样品相比,处理后的样品的比表面积显著增加了9.8%。处理后样品的融合潜热和分解潜热分别较对照样品显著提高11.71%和123.52%。总减重显著降低10.59%;但处理后的氧氟沙星与对照相比,其残留量显著增加了63.29%。Trivedi效应®-意识能量愈合治疗产生了一种新的多形性氧氟沙星,与未经处理的样品相比,它可能更容易溶解,生物利用度更高,热稳定性更强。治疗后的氧氟沙星对蜂窝组织炎、前列腺炎、慢性支气管炎、尿路感染、尿道和宫颈感染、肺炎、传染性腹泻、鼠疫等更有效。
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引用次数: 0
Impact of Recent Trends in Drug Discovery and Development 药物发现和开发最新趋势的影响
Pub Date : 2019-01-01 DOI: 10.19080/omcij.2019.08.555735
Neema Bisht, A. Sah
Discovery and development of a new drug is a very complex process as it takes long duration and various resources. The practice of drug discovery has been speeding up with the use of newer advanced techniques to increase the efficiency of the process. Various recent technologies like bioinformatics, computer-aided drug design (CADD), combinatorial chemistry has considerably extended its range of applications and spanning almost all stages in the drug discovery process. Chemical compounds can be screened out for their biological activity with target through high-throughput screening (HTS). Advanced technologies are using successfully now days due to speed up, low expenses and greater success rates in drug development. The main objective of this mini review is to highlight the utility of various recent trends in drug discovery.
新药的发现和开发是一个非常复杂的过程,需要较长的时间和多种资源。药物发现的实践已经加速使用新的先进技术,以提高效率的过程。最近的各种技术,如生物信息学、计算机辅助药物设计(CADD)、组合化学已经大大扩展了其应用范围,并跨越了药物发现过程的几乎所有阶段。通过高通量筛选(high-throughput screening, HTS)可以筛选出化合物与靶标的生物活性。由于药物开发速度快、费用低、成功率高,先进技术目前正在成功应用。这篇迷你综述的主要目的是强调药物发现中各种最新趋势的效用。
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引用次数: 1
Spectroscopic Evaluation of Novel TacrineCoumarin Hybrids as HSA-Interacting Agents 新型他克林-香豆素杂交种作为hsa相互作用剂的光谱评价
Pub Date : 2019-01-01 DOI: 10.19080/omcij.2019.08.555733
M. Kožurková
In this work, we investigated the human serum albumin binding behavior of a series of novel derivatives with both tacrine and coumarin pharmacophores. The compounds were investigated using UV-Vis absorption and fluorescence spectroscopy. KB values were found to be in order of 103 M-1. The values of n indicate that only one independent class of binding sites is available for tacrine-coumarin hybrids on HSA. Synchronous fluorescence spectra showed that compounds did not have any noticeably effect on α-helical conformation of HSA. Our data indicated that these tacrine-coumarin molecules exhibit promising potential which would be of considerable use in the development of drugs with enhanced or more selective effects and greater clinical efficacy.
在这项工作中,我们研究了一系列新的衍生物与他克林和香豆素药效团的人血清白蛋白结合行为。用紫外-可见吸收光谱和荧光光谱对化合物进行了研究。KB值约为103 M-1。n的值表明,在HSA上,他克林-香豆素杂种只有一类独立的结合位点。同步荧光光谱显示化合物对HSA的α-螺旋构象没有明显影响。我们的数据表明,这些他克林-香豆素分子在开发具有增强或更强选择性作用和更高临床疗效的药物方面具有很大的潜力。
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引用次数: 4
Synthesis, Characterization and Cytotoxic Studies of New Thiazolidinones 新型噻唑烷酮的合成、表征及细胞毒性研究
Pub Date : 2018-10-09 DOI: 10.19080/omcij.2018.08.555730
Ayaz Mahmood Dar
A new series of substituted aromatic thiazolidinones [1-4]were synthesized by the reaction of acetophenone and its derivatives [5-8]with hydrazine hydrate and merceptoacetic acid in absolute ethanol in one pot manner. The striking feature of this reaction is the formation of hydrazone in situ which in turn undergoes the cyclization with mercepto acetic acid, leading to the formation of new thiazolidinones. Thus, the thiazolidinone ring closes at carbonyl carbon, by the attack of sulfur of mercaptoacetic acid moiety, preferentially from the front (β, axial) so that the nitrogen has an equatorial orientation (α, equatorial) to avoid steric repulsion, giving minimum steric hindrance. The new compounds were characterized by spectral (IR, 1 H NMR, 13 C NMR, MS) and analytical methods. The new compounds were screened for cytotoxicity (MTT assay) as well as genotoxicity (Comet assay) studies against different cancer cell lines, during which the new compounds depicted potential anticancer behaviour.
以苯乙酮及其衍生物[5-8]与水合肼和巯基乙酸在无水乙醇中一锅反应合成了一系列新的取代芳香噻唑烷酮[1-4]。该反应的显著特点是在原位生成腙,而腙又与巯基乙酸发生环化反应,生成新的噻唑烷酮。因此,噻唑烷酮环受到巯基乙酸部分的硫的攻击,优先从前面(β,轴向)关闭,使氮具有赤道取向(α,赤道),以避免位阻,产生最小的位阻。通过红外光谱(IR)、核磁共振(1h NMR)、核磁共振(13c NMR)、质谱(MS)和分析方法对化合物进行了表征。新化合物对不同的癌细胞系进行了细胞毒性(MTT试验)和遗传毒性(Comet试验)研究,在此期间,新化合物描绘了潜在的抗癌行为。
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引用次数: 0
Synthesis of Substituted Quinazolines Containing Pharmacophoric Groups 含药效基团取代喹唑啉类化合物的合成
Pub Date : 2018-10-01 DOI: 10.19080/omcij.2018.08.555729
Harutyunyan Artur A
Continuing research on the synthesis of biologically active quinazoline derivatives [1,2] in this report we have described the synthesis of previously unknown substituted 2-methylquinzolins and 2-[2-aryl(hetaryl)vinyl]quinazolines, which contain pharmacophore groups at different positions of the ring. Synthesis was carried out by the interaction of 2-methyl-4H-3,1-benzoxzin4-ones 1a, b with aromatic and heterocyclic amines, according to the Scheme 1.
对生物活性喹唑啉衍生物合成的持续研究[1,2]在本报告中,我们描述了以前未知的取代2-甲基喹唑啉和2-[2-芳基(己基)乙烯基]喹唑啉的合成,它们在环的不同位置含有药效团。2-甲基- 4h -3,1-苯并恶辛- 1,1a, b与芳香胺和杂环胺相互作用,按照方案1进行合成。
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引用次数: 1
Molecular Structure of Metal Complexes of Certain Benzimidazole Derivatives 某些苯并咪唑衍生物金属配合物的分子结构
Pub Date : 2018-09-28 DOI: 10.19080/omcij.2018.08.555728
Manjunatha M N
using MoKα (0.71073 Å) radiation for the crystal. Intensity data was collected up to a max of 26.81° for the compound in the w–ф scan mode. The data was reduced using SAINTPLUS [8].
利用MoKα (0.71073 Å)辐射对晶体进行分析。在w - w扫描模式下,化合物的强度数据最大可达26.81°。使用SAINTPLUS[8]减少数据量。
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引用次数: 0
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Organic & Medicinal Chemistry International Journal
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