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Functionalization of semi-conductive interfaces with cucurbit[n]urils 用葫芦[n]脲使半导电界面功能化
IF 2.3 4区 化学 Q2 Chemistry Pub Date : 2024-01-05 DOI: 10.2174/0118756298232086231203163938
Andisiwe Ngwekazi, Christopher Arendse, Priscilla Baker
: Cucurbiturils are a class of macrocyclic compounds with highly polar carbonyl portals and a hydrophobic cavity. They are usually utilized as efficient host molecules in supramolecular chemistry applications due to their high binding affinity for positively charged or cationic compounds. This review investigates the application of CB[n] immobilization at semi-conductive interfaces to produce electrochemical sensors. Critical to the production of thin film electrode preparations is the solubility of the CB[n] to produce homogeneous thin films when deposited. The solubility of CB[n] molecules in organic and inorganic solvents is limited; however, CB[7] has been applied successfully in the production of a wide range of electrochemical sensors. Furthermore, we introduce simple drop-casting of efficiently solubilized CB[7] as a simple yet effective method for producing CB[7] modified electrochemical sensors for the sensitive reporting of dopamine in aqueous solutions in the concentration range of 3.33×10-9 to 1.16×10-8 M with a sensitivity of 0.315 µA/M, (n=3).
:葫芦脲是一类具有高极性羰基门户和疏水空腔的大环化合物。由于它们与带正电荷或阳离子的化合物具有很高的结合亲和力,因此在超分子化学应用中通常被用作高效的宿主分子。本综述探讨了如何将 CB[n] 固定在半导电界面上以生产电化学传感器。薄膜电极制备的关键是 CB[n] 的溶解度,以便在沉积时产生均匀的薄膜。CB[n] 分子在有机和无机溶剂中的溶解度有限,但 CB[7] 已成功应用于生产各种电化学传感器。此外,我们还介绍了一种简单而有效的方法,即利用高效溶解的 CB[7] 进行简单的液滴浇铸,来生产 CB[7] 改性电化学传感器,用于灵敏地报告水溶液中多巴胺的浓度,浓度范围为 3.33×10-9 至 1.16×10-8M,灵敏度为 0.315 µA/M(n=3)。
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引用次数: 0
Recent Advances in the Construction of Coumarin or Quinolin-2-ones Compounds via Radical Cascade Reactions 通过自由基级联反应构建香豆素或 2-喹啉酮化合物的最新进展
IF 2.3 4区 化学 Q2 Chemistry Pub Date : 2024-01-05 DOI: 10.2174/0118756298278048231205053801
Shuo Zhang, Wei Tang, Kai Zhou, Xiao-Xiao Huan, Zhi-Wei Chen
: Free radical reactions occupy an important position in synthetic organic chemistry as well as medicinal chemistry, significantly complementing and extending the synthesis of coumarin or quinolin-2-one compounds. Moreover, the use of constructing coumarin or quinolin-2-one compounds functionalized at the C3 position has certain advantages over traditional noble metalcatalyzed or high-temperature cyclization, which is more in line with the advocates of green chemistry. The design of alkenes or alkynes as radical acceptors for cascade reactions presents a novel and robust approach to obtaining coumarin or quinolin-2-one molecules. These radical cascade cyclization reactions have been well explored and studied over the past decade. As a result, we have compiled a review of the rapidly developing cutting-edge research in this field, featuring typical examples and in-depth exploration of the underlying mechanisms.
:自由基反应在合成有机化学和药物化学中占有重要地位,极大地补充和扩展了香豆素或喹啉-2-酮化合物的合成。此外,与传统的贵金属催化或高温环化相比,利用 C3 位功能化构建香豆素或喹啉-2-酮化合物具有一定的优势,更符合绿色化学的主张。设计烯烃或炔烃作为级联反应的自由基受体,是获得香豆素或喹啉-2-酮分子的一种新颖而稳健的方法。在过去十年中,这些自由基级联环化反应得到了充分的探索和研究。因此,我们汇编了该领域快速发展的前沿研究综述,其中包括典型实例和对基本机理的深入探讨。
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引用次数: 0
Meet the Editorial Advisory Board Member 与编辑顾问委员会成员会面
IF 2.3 4区 化学 Q2 Chemistry Pub Date : 2023-11-01 DOI: 10.2174/1570193x2007230331134915
I. Iavicoli
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引用次数: 0
Asciminib - ABL Kinase Inhibitor in the Treatment of Philadelphia Chromosome Positive Chronic Myeloid Leukemia: Chemistry and Pharmacology Perspectives 阿西米尼- ABL激酶抑制剂治疗费城染色体阳性慢性髓性白血病:化学和药理学观点
4区 化学 Q2 Chemistry Pub Date : 2023-10-17 DOI: 10.2174/0118756298270515231010062046
Umang Shah, Prachi Patel, Alkesh Patel, Dhruvi Gajjar, Mehul Patel, Nilay Solanki, Swayamprakash Patel, Ashish Patel, Rajesh Maheshwari
Abstract: Asciminib, also known as ACP-196, is the FDA-approved low-molecular ABL kinase inhibitor. The ABL kinase is a non-receptor tyrosine kinase that helps in cell growth and survival and is a key player in the development of chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ALL). The BCR-ABL fusion protein, which is formed by chromosomal translocation in CML and Ph+ ALL, results in the constitutive activation of ABL kinase, leading to uncontrolled cell growth and proliferation. To have a high binding affinity for the active site of the enzyme, structural biology and computer-aided drug design (CADD) concepts were applied to the design of asciminib so that it could specifically target the ABL kinase enzyme. The drug was synthesized and characterized in a laboratory. In its pharmacological studies, it has shown that asciminib is a potent and selective inhibitor of ABL kinase. Phase I clinical trials assessed its safety and efficacy, revealing that it is effective against tumors while causing minimal discomfort to patients. In addition to this, it was able to induce apoptosis and a cytogenetic response as well as inhibit the proliferation of CML and Ph+ALL cells in patients with CML. As this trial gave a positive response, phase II and III trials were conducted. In that sense, asciminib has shown to be highly effective, with response rates of over 90% in patients with these diseases. The safety and efficacy of asciminib were also evaluated in combination with other drugs, such as tyrosine kinase inhibitors and immunomodulatory drugs, and the results were promising. Overall, the discovery and development of asciminib showed that by using the concepts of pharmacology and CADD, a drug with a 90% positive rate response can be developed with a high tolerance level and lower side effects
摘要:Asciminib,又称ACP-196,是fda批准的低分子ABL激酶抑制剂。ABL激酶是一种非受体酪氨酸激酶,有助于细胞生长和存活,在慢性髓性白血病(CML)和费城染色体阳性急性淋巴细胞白血病(Ph+ALL)的发展中起关键作用。BCR-ABL融合蛋白在CML和Ph+ ALL中通过染色体易位形成,导致ABL激酶的组成性激活,导致细胞生长和增殖失控。为了对酶的活性位点具有高结合亲和力,我们将结构生物学和计算机辅助药物设计(CADD)的概念应用于阿西米尼的设计,使其能够特异性靶向ABL激酶酶。这种药物是在实验室合成并鉴定的。药理研究表明,阿西米尼是一种有效的选择性ABL激酶抑制剂。I期临床试验评估了它的安全性和有效性,表明它对肿瘤有效,同时对患者的不适最小。除此之外,它还能诱导细胞凋亡和细胞遗传学反应,抑制CML和Ph+ALL细胞在CML患者中的增殖。由于该试验获得了积极的反应,因此进行了II期和III期试验。从这个意义上说,阿西米尼已被证明是非常有效的,在患有这些疾病的患者中,反应率超过90%。阿西米尼与其他药物如酪氨酸激酶抑制剂和免疫调节药物联合使用的安全性和有效性也进行了评价,结果是有希望的。总的来说,阿西米尼的发现和开发表明,利用药理学和CADD的概念,可以开发出一种阳性率为90%、耐受性高、副作用小的药物
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引用次数: 0
Xanthates and Dithiocarbamates: Synthesis, Characterization and Application in Flotation Processes 黄原酸盐和二硫代氨基甲酸盐:合成、表征及其在浮选中的应用
4区 化学 Q2 Chemistry Pub Date : 2023-10-10 DOI: 10.2174/0118756298267964231004113212
Nadezhda V. Vchislo, Ekaterina A. Verochkina, Igor B. Rozentsveig, Alexander E. Burdonov
Abstract: It is known that flotation is the main method of extracting non-ferrous metals. The need of modern society for precious metals is constantly growing, and deposits of easily reversible ores are being depleted. Therefore, the improvement of the reagent regime and the search for new flotation reagents is an urgent task. We analyzed the literature data on the synthesis and use of common collectors such as xanthates and dithiocarbamates. Particular importance is given to recent progress in the functionalization of xanthates and dithiocarbamates, their selective characteristics and flotation mechanisms. Progress in the field of flotation can be made in the use of new effective reagents and their combinations, as well as in the modification of already known collectors. The generalization of the material in this review will help in the development of this area. The mini-review summarizes the syntheses of collectors such as xanthates and dithiocarbamates with the increased selective properties in the flotation process of non-ferrous metals. Furthermore, this review provides an analysis of the developments in these studies, especially highlighting recent progress in the functionalization of xanthates and dithiocarbamates, their selective characteristics and flotation mechanisms.
摘要:浮选是提取有色金属的主要方法。现代社会对贵金属的需求不断增长,而易于回收的矿石储量正在枯竭。因此,改善药剂制度和寻找新的浮选药剂是一项紧迫的任务。对黄原酸盐和二硫代氨基甲酸盐等常用捕收剂的合成和使用进行了文献分析。特别重视黄原酸盐和二硫代氨基甲酸盐功能化的最新进展,它们的选择特性和浮选机制。浮选领域的进展可以在使用新的有效药剂及其组合以及对已知捕收剂进行改性方面取得进展。本文对材料的归纳将有助于这一领域的发展。综述了黄原酸盐和二硫代氨基甲酸盐等捕收剂在有色金属浮选过程中选择性增强的合成情况。此外,本文还对黄原酸盐和二硫代氨基甲酸盐的功能化、选择性和浮选机理等方面的研究进展进行了综述。
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引用次数: 0
Introduction to a New Technique in Organic Synthesis: Recent Advances in Aqueous Reactions of Sparingly Soluble High-Melting Point Substrates Promoted by Granular Polytetrafluoroethylene 有机合成新技术简介:颗粒聚四氟乙烯促进高熔点稀溶底物的水反应研究进展
4区 化学 Q2 Chemistry Pub Date : 2023-10-05 DOI: 10.2174/0118756298253318230929034500
Linlin Xing, Yong Zhang, Taixuan Jia, Chunbao Li
Abstract: Water, a kind of abundant natural resource, is considered to be a green and desirable solvent for reasons of its low cost, high safety and environmental friendliness. This review article aims to briefly introduce the methodologies that have utilized water as reaction media under the aid of granular polytetrafluoroethylene (PTFE) to mediate reactions of a series of water-insoluble and high melting points substrates in a green, quantitative, fast, and stereoselective way in most situations. Besides, this review will be helpful to stimulate further study on both practical applications and mechanistic understanding of these aqueous reactions promoted by granular PTFE for the novel synthesis of interesting structures.
摘要:水作为一种丰富的自然资源,因其成本低、安全性高、环境友好而被认为是一种绿色、理想的溶剂。本文简要介绍了在颗粒聚四氟乙烯(PTFE)的辅助下,利用水作为反应介质,在大多数情况下以绿色、定量、快速和立体选择性的方式介导一系列水不溶性和高熔点底物的反应的方法。此外,本文的综述将有助于进一步研究颗粒聚四氟乙烯促进这些水反应的实际应用和机理,以合成新的有趣的结构。
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引用次数: 0
Photochemistry of Riboflavin: The Primary Transients 核黄素的光化学:初级瞬态
4区 化学 Q2 Chemistry Pub Date : 2023-09-13 DOI: 10.2174/1570193x21666230913092924
Igor V. Khudyakov
Abstract: Primary photoreactions of riboflavin (Rf) are considered. The goal was to present data on the transients formed under photoexcitation of Rf: excited singlet and triplet states, triplet reactions with the formation of Rf neutral free radicals, and a radical anion. The absorption spectra of transients are presented, as are the rate constants of their decay. Special attention is devoted to Rf in water (aerobic and anaerobic reactions).
摘要:研究了核黄素(Rf)的初级光反应。目的是提供在Rf光激发下形成的瞬态数据:激发单线态和三重态,三重态反应与Rf中性自由基的形成,以及自由基阴离子。给出了瞬态的吸收光谱,以及它们衰变的速率常数。特别关注水中的Rf(好氧和厌氧反应)。
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引用次数: 0
Synthetic Approaches and Reactions of 2-(Arylidene)benzo[b]thiophen-3(2H)one-1,1-dioxides 2-(芳基)苯并[b]噻吩-3(2H) 1- 1,1-二氧化物的合成方法及反应
4区 化学 Q2 Chemistry Pub Date : 2023-09-06 DOI: 10.2174/1570193x21666230906141749
RAJ KUMAR, Subrata Barick, Manvendra Kumar
Abstract: 2-(Arylidene)benzo[b]thiophen-3(2H)one 1,1-dioxides are oxidized form of thioaurones. Various methods have been reported for their synthesis, e.g., a) condensation of benzo[b]thiophen-3(2H)one 1,1-dioxides with aryl aldehydes under acidic or basic conditions, b) oxidation of thioaurones with hydrogen peroxide or sodium perborate tetrahydrate, c) from the catalytic reaction of iodonium ylides with (bis(trifluoroacetoxy)iodo) benzene in presence copper(II)acetoacetonate, d)by ring contraction of 1-thioflavones in the presence of ceric ammonium nitrate. The reports have shown addition reactions with p-thiocresol in the absence of any catalyst, conjugated addition product without hetero ring opening with Grignard reagent, forms corresponding oxime and hydrazone with hydroxyl amine and phenyl hydrazine, respectively, produces polycyclic compounds with enamines, shows contrasting behavior with NBS and gives addition products with organophosphorus compounds in both hydroxylic and non-hydroxylic solvents which depends on reaction medium. In the present mini-review, we have discussed the various synthetic strategies and reactions of 2-(arylidene)benzo[b]thiophen-3(2H)one 1,1-dioxides, along with their reported utilities.
摘要:2-(芳基)苯并[b]噻吩-3(2H) 1,1-二氧化物是硫芴酮的氧化形式。它们的合成方法有多种,例如:a)苯并[b]噻吩-3(2H) - 1,1-二氧化物与芳基醛在酸性或碱性条件下缩合,b)用过氧化氢或四水合过硼酸钠氧化硫酮,c)在铜的存在下碘化物与(二(三氟乙酰氧基)碘)苯的催化反应(II)乙酰丙酮,d)在硝酸铈铵的存在下通过1-硫黄酮的环收缩。报道了与对硫甲酚在无催化剂条件下的加成反应,与格氏试剂无杂环开孔的共轭加成产物,分别与羟胺和苯基肼生成相应的肟和腙,与胺生成多环化合物,与NBS表现出对比行为,并与有机磷化合物在羟基和非羟基溶剂(取决于反应介质)中生成加成产物。在这篇综述中,我们讨论了2-(芳基)苯并[b]噻吩-3(2H) 1,1-二氧化物的各种合成策略和反应,以及它们的应用报道。
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引用次数: 0
Natural Existence and Bioactivity of Flavonoids: Synthetic Strategies and Mechanistic Pathways 黄酮类化合物的天然存在和生物活性:合成策略和机制途径
IF 2.3 4区 化学 Q2 Chemistry Pub Date : 2023-09-01 DOI: 10.2174/1570193x21666230901110030
Shivangi Sharma, Pankaj Kumar Mishra, Shivendra Singh
A class of chemicals known as flavonoids is widely distributed in various portions of plants, cereals, and vegetables. They have varied phenolic structures and these flavonoid molecules are known for the well-being improvement in living things. Today, a wide range of pharmaceutical, medicinal, & cosmetic materials possessed these key ingredients, known as flavonoids. Flavonoids can modulate the bioactivity of essential enzymes & their properties such as anti-mutagenic, anti-inflammatory, anti-oxidative, & anti-carcinogenic. The current patterns of flavonoid in research & development helps in the identification, isolation, characterization, & functions of flavonoids as well as their applications for better biological activities. In this article, we have discussed the natural existence and structural frameworks of the different classes of potential bioactive flavonoids. In addition to this, different synthetic strategies, and their mechanistic pathways for the preparation of different classes of flavonoids are also discussed thoroughly here. Owing to its tremendous natural existence and bioactivity, more research is still needed to further explore the usefulness of flavonoids for human wellness. The major challenge with the study of such flavonoids is the diversity of molecular structures & scarcity of data on their bioavailability. However, this article will be helpful for understanding the chemical aspect and several potential bioactivities of flavonoids
黄酮类化合物广泛分布于植物、谷物和蔬菜的各个部位。它们具有不同的酚类结构,这些类黄酮分子对改善生物的健康状况是已知的。如今,各种各样的药物、医药和化妆品材料都含有这些关键成分,即黄酮类化合物。黄酮类化合物可以调节必需酶的生物活性及其抗突变、抗炎、抗氧化和致癌等特性。黄酮类化合物目前的研究和开发模式有助于黄酮类化合物的鉴定、分离、表征和功能,以及它们在更好的生物活性方面的应用。在这篇文章中,我们讨论了不同种类的潜在生物活性黄酮的天然存在和结构框架。除此之外,本文还深入讨论了不同的合成策略及其制备不同类别黄酮类化合物的机理途径。由于类黄酮具有巨大的天然存在和生物活性,还需要更多的研究来进一步探索类黄酮对人类健康的有用性。研究此类黄酮类化合物的主要挑战是分子结构的多样性和生物利用度数据的匮乏。然而,这篇文章将有助于理解类黄酮的化学方面和几种潜在的生物活性
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引用次数: 0
A Review on Synthesis, Characterization, and Pharmacological Properties of Some Sydnone Derivatives 一些syd酮衍生物的合成、表征及药理性质的研究进展
IF 2.3 4区 化学 Q2 Chemistry Pub Date : 2023-08-31 DOI: 10.2174/1570193x21666230831153810
T. Khan, Ritu Yadav, A. K. Kesharwani, Karuna Chourasia
The mesoionic compounds have great importance due to their dipolar nature. They are versatile synthons in synthetic chemistry and possess various chemotherapeutic activities. The most important moiety found in mesoionic compounds is the sydnone ring system. Sydnone derivatives have stimulated much interest among synthetic researchers as a result of their unique dipolar, mesoionic character. This ring system is also associated with a wide variety of biological activities. Sydnone derivatives have various applications in synthetic and medicinal chemistry. Sydnones are very useful precursors for selective heterocycles (pyrazoles, imidazoles, oxadiazoles, oxazoles, thiazoles, and tetrazoles), which has also served to initiate research into their functionalization and cycloaddition chemistry, paving the way for stimulated extensive research on the use of sydnones in chemical and industrial applications. So, this review article offers a wide scope of synthesis and applications of sydnone derivatives.
介电离子化合物由于其偶极性质而具有重要意义。它们是合成化学中的多功能合成子,具有多种化学治疗活性。在介电离子化合物中发现的最重要的部分是sydnone环系统。Sydnone衍生物由于其独特的偶极、介电性质而引起了合成研究人员的极大兴趣。这个环状系统还与各种各样的生物活动有关。Sydnone衍生物在合成化学和药物化学中有各种应用。Sydnone是选择性杂环(吡唑、咪唑、恶二唑、恶唑、噻唑和四唑)的非常有用的前体,这也有助于启动对其功能化和环加成化学的研究,为促进Sydnone在化学和工业应用中的广泛研究铺平了道路。因此,本文对sydnone衍生物的合成和应用进行了综述。
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引用次数: 0
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Mini-reviews in Organic Chemistry
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