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Ionic Liquid-promoted the Synthesis of Structurally Diverse Pyrans, Pyranannulated Heterocycles, and Spiropyrans 离子液体促进结构多样的吡喃、吡喃杂环和螺吡喃的合成
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-03-19 DOI: 10.2174/0113852728300880240223063813
Bubun Banerjee, Manmeet Kaur, Anu Priya, Aditi Sharma, Arvind Singh
: During the last two decades, non-conventional solvents, especially various ionic liquids, have been utilized as efficient reaction media as they can play a dual role as solvents and promoters. The use of ionic liquids as a medium increases the efficiency of the reactions due to their inherent features like high thermal stability, ability to act as a catalyst, non-volatility, high polarity, reusability, ability to dissolve a large number of organic and inorganic compounds, etc. Under this direction, various structurally diverse ionic liquids have been employed as efficient reaction media for various organic transformations. On the other hand, among many other important synthetic scaffolds, during the last two decades, the synthesis of pyrans, pyran-annulated heterocyclic scaffolds, and spiropyrans have gained huge attention as they possess a wide range of significant biological efficacies, which include antibacterial, anticancer, antimycobacterial, antioxidant, xanthine oxidase inhibitory, etc. activities. Almost every day, many new methods are being added to the literature related to synthesizing pyrans, pyran-annulated heterocyclic scaffolds, and spiropyrans. Among many other alternatives, various ionic liquids have also played an efficient role as promoters for synthesizing structurally diverse pyrans, pyranannulated heterocyclic scaffolds, and spiropyrans. In this review, we have summarized a large number of literature reported during the last two decades related to the ionic liquid-promoted synthesis of pyrans, pyranannulated heterocyclic scaffolds, and spiropyran derivatives.
:在过去的二十年里,非常规溶剂,尤其是各种离子液体,被用作高效的反应介质,因为它们可以发挥溶剂和促进剂的双重作用。离子液体具有热稳定性高、可用作催化剂、不挥发、极性强、可重复使用、可溶解大量有机和无机化合物等固有特性,因此使用离子液体作为介质可提高反应效率。在此指导下,各种结构各异的离子液体已被用作各种有机转化的高效反应介质。另一方面,在许多其他重要的合成支架中,近二十年来,吡喃、吡喃annulated杂环支架和螺环吡喃的合成受到了极大关注,因为它们具有广泛而显著的生物功效,包括抗菌、抗癌、抗霉菌、抗氧化、抑制黄嘌呤氧化酶等活性。几乎每天都有许多与合成吡喃、吡喃annulated杂环支架和螺吡喃有关的新方法出现在文献中。在许多其他替代方法中,各种离子液体也在合成结构多样的吡喃、吡喃杂环支架和螺环吡喃中发挥了有效的促进作用。在本综述中,我们总结了过去二十年中有关离子液体促进合成吡喃、吡喃杂环支架和螺吡喃衍生物的大量文献。
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引用次数: 0
3D Printing Chitosan-based Nanobiomaterials for Biomedicine and Drug Delivery: Recent Advances on the Promising Bioactive Agents and Technologies 三维打印壳聚糖基纳米生物材料用于生物医学和药物输送:前景看好的生物活性剂和技术的最新进展
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-03-19 DOI: 10.2174/0113852728298168240222114449
Seyed Morteza Naghib, Morteza Zarrineh, M. R. Mozafari
: 3D bioprinting is a novel technology that has gained significant attention recently due to its potential applications in developing simultaneously controlled drug delivery systems (DDSs) for administering several active substances, such as growth factors, proteins, and drug molecules. This technology provides high reproducibility and precise control over the fabricated constructs in an automated way. Chitosan is a naturalderived polysaccharide from chitin, found in the exoskeletons of crustaceans such as shrimp and crabs. Chitosan- based implants can be prepared using 3D bioprinting technology by depositing successive layers of chitosan- based bioink containing living cells and other biomaterials. The resulting implants can be designed to release drugs at a controlled rate over an extended period. The use of chitosan-based implants for drug delivery has several advantages over conventional drug delivery systems. Chitosan is biodegradable and biocompatible, so it can be safely used in vivo without causing any adverse effects. It is also non-immunogenic, meaning it does not elicit an immune response when implanted in vivo. Chitosan-based implants are also costeffective and can be prepared using simple techniques. 3D bioprinting is an emerging technology that has revolutionized the field of tissue engineering by enabling the fabrication of complex 3D structures with high precision and accuracy. It involves using computer-aided design (CAD) software to create a digital model of the desired structure, which is then translated into a physical object using a 3D printer. The printer deposits successive layers of bioink, which contains living cells and other biomaterials, to create a 3D structure that mimics the native tissue. One of the most promising applications of 3D bioprinting is developing drug delivery systems (DDSs) to administer several active substances, such as growth factors, proteins, and drug molecules. DDSs are designed to release drugs at a controlled rate over an extended period, which can improve therapeutic efficacy and reduce side effects. Chitosan-based implants have emerged as a promising candidate for DDSs due to their attractive properties, such as biodegradability, biocompatibility, low cost, and nonimmunogenicity. 3D bioprinting technology has emerged as a powerful tool for developing simultaneously controlled DDSs for administering several active substances. The rationale behind integrating 3D printing technology with chitosan-based scaffolds for drug delivery lies in the ability to produce customized, biocompatible, and precisely designed systems that enable targeted and controlled drug release. This novel methodology shows potential for advancing individualized healthcare, regenerative treatments, and the creation of cutting- edge drug delivery systems. This review highlights the potential applications of 3D bioprinting technology for preparing chitosan-based implants for drug delivery.
三维生物打印技术是一种新型技术,最近因其在开发可同时控制的给药系统(DDS)以给药多种活性物质(如生长因子、蛋白质和药物分子)方面的潜在应用而备受关注。这种技术具有很高的可重复性,并能以自动化方式精确控制制造的结构。壳聚糖是从甲壳素中提取的天然多糖,存在于虾蟹等甲壳类动物的外骨骼中。使用三维生物打印技术可以制备以壳聚糖为基础的植入物,方法是连续沉积含有活细胞和其他生物材料的以壳聚糖为基础的生物墨水层。设计出的植入物可在较长时间内以可控速率释放药物。与传统的给药系统相比,使用壳聚糖基植入物给药具有多项优势。壳聚糖具有生物降解性和生物相容性,因此可以在体内安全使用,不会造成任何不良影响。此外,它还具有非免疫原性,这意味着在体内植入时不会引起免疫反应。壳聚糖基植入物还具有成本效益,可以用简单的技术制备。三维生物打印技术是一项新兴技术,通过高精度、高准确度地制造复杂的三维结构,彻底改变了组织工程领域。它包括使用计算机辅助设计(CAD)软件创建所需结构的数字模型,然后使用三维打印机将其转化为实物。打印机连续沉积含有活细胞和其他生物材料的生物墨水层,以创建模仿原生组织的三维结构。三维生物打印最有前途的应用之一是开发药物输送系统(DDS),以输送多种活性物质,如生长因子、蛋白质和药物分子。DDS 的设计目的是在较长时间内以可控速率释放药物,从而提高疗效并减少副作用。壳聚糖基植入物具有生物可降解性、生物相容性、低成本和非免疫原性等诱人特性,因此已成为 DDSs 的理想候选材料。三维生物打印技术已成为开发可同时控制多种活性物质给药的 DDSs 的有力工具。将三维打印技术与壳聚糖基支架整合用于给药的理由在于,该技术能够生产出定制化、生物相容性和精确设计的系统,从而实现有针对性的可控药物释放。这种新颖的方法显示出推动个性化医疗保健、再生治疗和创建尖端给药系统的潜力。本综述重点介绍了三维生物打印技术在制备基于壳聚糖的给药植入物方面的潜在应用。
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引用次数: 0
Synthesis, Molecular Docking, Anti-cholinesterase Activity, Theoretical Investigation, and Catalytic Effect of New Encumbered N-benzyladamantyl Substituted Imidazolidin-2-ylidene Carbene Pd-PEPPSI Complexes N-苄基-2-咪唑烷基-2-亚基碳烯 Pd-PEPPSI 新包合物的合成、分子对接、抗胆碱酯酶活性、理论研究和催化作用
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-03-19 DOI: 10.2174/0113852728289791240222054306
Sofiane ikhlef, Sarra Lasmari, Saber Mustapha Zendaoui, El Hassen Mokrani, Dahmane Tebbani, Nevin Gürbüz, Chawki Bensouici, Raouf Boulcina, Bachir Zouchoune, Ismail Özdemir
: This study aimed to describe the preparation of novel PEPPSI type Pd(II)-NHC complexes bearing N-benzyladamantyl substituted imidazolidin-2-ylidene group. All synthesized compounds were characterized by using 1 H-NMR and 13C-NMR spectroscopies, FTIR, and elemental analysis techniques. One of the objectives of this study was the synthesis of Pd-NHC complexes with AChE/BChE inhibition activities. Among all the tested compounds, complexes 4b and 4c were found to have the most high potential AChE and BChE inhibitory activities with IC50 values of 21.57 ± 0.23 Mm and 15.78 ± 0.39 Mm, respectively. Conducting molecular docking studies helped us in gathering crucial information about the main binding interactions of inhibitors and enzymes, and the results were in agreement with the biological evaluation. The synthesized Pd-NHC complexes were employed for catalyzing the direct C2- and C5-arylation reaction between aryl (hetero) halide and a variety of heterocyclic systems. In both cases (C2 and C5-arylation), Pd-NHC complexes catalysts provided access to the arylated heterocycles in good to high yields in the presence of 1 mol% catalyst loading at 150 °C. The DFT theoretical investigation showed that the Pd-NHC complexes were of ML2X2 type, where the the Pd(II) cation had a square planar geometry. The interaction energies obtained by energy decomposition analysis (EDA) demonstrated that the 4d and 4e complexes were more stable in the presence of more methyl substituents. The chemical indicators demonstrated that the less stable 4c complex was more reactive in regard to the chemical hardness, chemical potential, and electrophilicity values.
:本研究旨在描述新型 PEPPSI 型 Pd(II)-NHC 配合物的制备过程,这些配合物带有 N-苄基氨基甲酰基取代的咪唑烷-2-亚基。利用 1 H-NMR 和 13C-NMR 光谱、傅立叶变换红外光谱以及元素分析技术对所有合成化合物进行了表征。本研究的目标之一是合成具有 AChE/BChE 抑制活性的 Pd-NHC 复合物。在所有测试化合物中,发现复合物 4b 和 4c 具有最强的潜在 AChE 和 BChE 抑制活性,其 IC50 值分别为 21.57 ± 0.23 Mm 和 15.78 ± 0.39 Mm。分子对接研究有助于我们收集抑制剂与酶的主要结合相互作用的关键信息,其结果与生物学评价一致。合成的 Pd-NHC 复合物被用于催化芳基(杂)卤化物与多种杂环体系之间的直接 C2 和 C5 芳基化反应。在这两种情况下(C2 和 C5-芳基化),Pd-NHC 配合物催化剂在 150 °C、催化剂负载量为 1 mol%的条件下,都能以良好到较高的产率获得芳基化杂环。DFT 理论研究表明,Pd-NHC 复合物属于 ML2X2 类型,其中 Pd(II) 阳离子具有正方形平面几何结构。通过能量分解分析(EDA)获得的相互作用能表明,甲基取代基越多,4d 和 4e 复合物越稳定。化学指标表明,稳定性较差的 4c 复合物在化学硬度、化学势和亲电性值方面反应性更强。
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引用次数: 0
One-Pot Multicomponent Synthesis of Pyrano[2,3-c]pyrazole and 2-Amino-4Hbenzo[ b]pyrans Catalyzed by Hercynite@SiO2@Tris as Novel and Efficient Nanocatalyst 新型高效纳米催化剂 Hercynite@SiO2@Tris 催化的吡喃并[2,3-c]吡唑和 2-氨基-4H-苯并[b]吡喃的一锅多组分合成反应
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-03-19 DOI: 10.2174/0113852728270373240222095835
Shima Beiranvand, Masoomeh Norouzi, Bahman Tahmasbi
: In this study, magnetic hercynite nanoparticles (FeAl2O4, MNPs) were functionalized by cheap and readily available tris(hydroxymethyl)aminomethane (Tris) as an organocatalyst. Various techniques, including Vibrating Sample Magnetometry (VSM), Energy Dispersive X-ray Spectroscopy (EDS), X-ray Diffraction (XRD), Scanning Electron Microscopy (SEM), and Thermogravimetric Analysis (TG) were employed to determine the morphology, particle size, physical properties, and magnetic properties of the nanoparticles. Additionally, Fourier transform infrared spectroscopy (FT-IR) techniques were used to investigate the presence of the functional group. The activity of this new catalyst as a magnetically recoverable nanocatalyst was investigated in the synthesis of oxygen and nitrogen-containing heterocyclic compounds. Pyranoprazole and 2-amino-4Hbenzo[ b]pyrans compounds were synthesized with high efficiency in a short time. FeAl2O4@SiO2@Tris can be separated using magnetic attraction and reused up to 5 consecutive times without a significant decrease in the yield of target products or catalytic activity.
:在这项研究中,磁性海泡石纳米颗粒(FeAl2O4,MNPs)被廉价易得的三(羟甲基)氨基甲烷(Tris)作为有机催化剂功能化。研究人员采用了多种技术,包括振动样品磁强计 (VSM)、能量色散 X 射线光谱仪 (EDS)、X 射线衍射 (XRD)、扫描电子显微镜 (SEM) 和热重分析 (TG),以确定纳米颗粒的形态、粒度、物理性质和磁性能。此外,还采用了傅立叶变换红外光谱(FT-IR)技术来研究官能团的存在。在合成含氧和含氮杂环化合物的过程中,研究了这种新型磁性可回收纳米催化剂的活性。在短时间内高效合成了吡喃拉唑和 2-氨基-4H-苯并[b]吡喃化合物。FeAl2O4@SiO2@Tris 可利用磁力吸引进行分离,并可连续重复使用多达 5 次,而目标产物的产率和催化活性不会明显降低。
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引用次数: 0
The Chemistry of Aldehydes and Ketones in the Synthesis of Heterocycles - Historical Reactions with a New and Green Perspective 杂环合成中的醛酮化学--以全新绿色视角看历史反应
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-03-19 DOI: 10.2174/0113852728295534240223044735
Flavia Martins da Silva, Joel Jones Junior, July A. Hernández Muñoz
: The reactivity of aldehydes and ketones carries great potential for multicomponent heterocyclizations. These reactions are convergent and highly versatile in the development of synthetic methodologies for compound families, displaying variations in substituents in their structures. Therefore, they have been regarded as an important tool in the field of Green Chemistry. Furthermore, they prove to be very useful in studies of biological activity, where small structural modifications can result in significant differences. Many heterocyclizations date back to the mid-19th and early 20th centuries. In this review, we aim to demonstrate, through some of these reactions, their continuously growing potential and improvements concerning synthetic development. Additionally, we present the original studies as reported, enabling us to appreciate the evolution of chemical representations over the years until reaching the standardization we have today.
:醛和酮的反应性为多组分杂环化带来了巨大的潜力。这些反应在化合物家族的合成方法开发方面具有趋同性和高度通用性,在其结构中显示出不同的取代基。因此,它们被视为绿色化学领域的重要工具。此外,它们在生物活性研究中也非常有用,因为在生物活性研究中,微小的结构改变也会导致显著的差异。许多杂环化反应可以追溯到 19 世纪中叶和 20 世纪初。在这篇综述中,我们旨在通过其中一些反应来展示它们不断增长的潜力以及在合成发展方面的改进。此外,我们还介绍了所报道的原始研究,使我们能够了解多年来化学表征的演变,直至今天的标准化。
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引用次数: 0
Facile Synthesis of 2-Substituted Quinazolines via Ruthenium(II)-Catalyzed Acceptorless Dehydrogenative Coupling 通过钌(II)催化的无受体脱氢偶联轻松合成 2-取代的喹唑啉类化合物
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-03-15 DOI: 10.2174/0113852728290175240213050011
Shulei Wu, Qianqian Lei, Zaoduan Wu, Huifang Xie, Chen Zhang, Yu Ye, Meiling Yi, Mingsheng Chen, Hao Xu, Zehua Yang
:: This study aims to develop a practical and facile one-pot synthesis of 2- substituted quinazolines. Using a commercially available and structurally simple ruthenium( II) complex as the catalyst to synthesize a series of quinazoline derivatives via acceptorless dehydrogenative coupling. The mechanism of this reaction was explored by control reaction and DFT calculation. This protocol offers access to a diverse array of quinazoline derivatives (52 examples) in moderate to excellent yields (29%-98%). In summary, we have developed an efficient one-pot ruthenium (II)-catalyzed ADC synthesis of quinazoline under an air atmosphere. The reaction only produces hydrogen and water as by-products, serving as a sustainable and atom-efficient synthetic approach.
::本研究旨在开发一种实用、简便的 2-取代喹唑啉类化合物的单锅合成方法。以一种市售的、结构简单的钌( II) 复合物为催化剂,通过无受体脱氢偶联合成一系列喹唑啉衍生物。通过控制反应和 DFT 计算探索了该反应的机理。该方法可以获得多种喹唑啉衍生物(52 例),产率从中等到极好(29%-98%)不等。总之,我们开发出了一种在空气气氛下高效的一锅钌 (II) 催化 ADC 合成喹唑啉的方法。该反应只产生氢气和水作为副产物,是一种可持续的原子高效合成方法。
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引用次数: 0
Recent Advances in Hypervalent Iodine Reagents and m-CPBA Mediated Oxidative Transformations 高价碘试剂和 m-CPBA 介导的氧化转化的最新进展
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-03-14 DOI: 10.2174/0113852728296345240215111730
Ravi Varala, Vittal Seema, Mohammed Amanullah, S. Ramanaiah, Mohammed Mujahid Allam
: Among the several peroxides available, meta-chloroperbenzoic acid (mCPBA) plays an efficient role of oxidizing reagent and is used for many oxidative transformations, such as oxidation of various functional groups, carbon-carbon, carbon-hetero bond formation, heterocyclic ring formation, heteroarylation, oxidative cross-coupling, lactonization, oxidative dearomatization, α-oxytosylation or α-acetoxylation, oxidative C-C bond activation and in other miscellaneous reactions. The purpose of this review is to critically discuss the significant contributions of mCPBA along with hypervalent iodine/iodine reagents in organic synthesis from mid-2015 to date.
:在现有的几种过氧化物中,间氯过苯甲酸(mCPBA)是一种高效的氧化试剂,可用于多种氧化转化,如各种官能团的氧化、碳-碳、碳-异键的形成、杂环的形成、杂芳基化、氧化交叉偶联、内酯化、氧化脱芳基化、α-氧代或α-乙酰氧代、氧化 C-C 键活化以及其他杂项反应。本综述旨在批判性地讨论 mCPBA 与高价碘/碘试剂自 2015 年年中至今在有机合成中的重大贡献。
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引用次数: 0
Investigation of the Role of Zirconia and Zirconia-containing Systems as Catalysts in Organic Transformations 研究氧化锆和含氧化锆体系作为有机转化催化剂的作用
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-03-14 DOI: 10.2174/0113852728290284240116042129
Kobra Nikoofar, Negin Shaddel, Fatemehsadat Jozi
: This review article discusses the applications of zirconia as a catalyst to promote various organic reactions and transformations. The article is subdivided into four main parts: 1) introduction, which consists of the history and introduction of zirconia, elaboration of its synthetic procedures, its application in various fields of science and technology with specified examples, and previously published review articles on ZrO2; 2) applications of sole zirconia and zirconia-based catalytic systems to promote various organic transformations, subdivided into oxidation reactions, hydrolysis and methanation reactions, reduction and hydrogenation reactions, furfural and synthesis of its derivatives, and miscellaneous reactions; 3) applications of sole zirconia and nanosized ZrO2 to catalyze organic reactions and MCRs, classified as two-component reactions, three-component reactions (by a glance at pseudo 3-CRs), and four-component reactions (by a glance at pseudo 4-CRs); and 4) applications of zirconia-containing catalytic systems to catalyze organic transformations and MCRs classified as two-component reactions, three-component reactions, and four-component and higher-component reactions. According to investigations, some of the zirconia-based catalysts exist in nano-sized systems. Moreover, the literature survey contains publications up to the end of July 2023.
:这篇综述文章讨论了氧化锆作为催化剂在促进各种有机反应和转化方面的应用。文章分为四个主要部分:1) 引言,包括氧化锆的历史和介绍、氧化锆合成过程的阐述、氧化锆在各个科技领域的应用(附具体实例)以及以前发表的有关 ZrO2 的综述文章;2) 单质氧化锆和氧化锆基催化体系在促进各种有机转化方面的应用,细分为氧化反应、水解和甲烷化反应、还原和氢化反应、糠醛及其衍生物的合成以及其他反应;3) 单氧化锆和纳米 ZrO2 催化有机反应和 MCR 的应用,分为双组分反应、三组分反应(通过伪 3-CR 一览)和四组分反应(通过伪 4-CR 一览);以及 4) 含氧化锆催化体系催化有机转化和 MCR 的应用,分为双组分反应、三组分反应和四组分及更高组分反应。根据调查,一些氧化锆基催化剂存在于纳米级系统中。此外,文献调查包含截至 2023 年 7 月底的出版物。
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引用次数: 0
Design, Synthesis, and Antimicrobial Evaluation of Novel Sulfonamide Modified with Azoles 用唑类修饰的新型磺酰胺的设计、合成和抗菌评估
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-03-14 DOI: 10.2174/0113852728296342240216074100
Pratibha Periwal, Ashwani Kumar, Vikas Verma, Devinder Kumar, Mahavir Parshad, Meenakshi Bhatia, Sourbh Thakur
Background:: Sulfonamide, imidazole, and triazole chemical nuclei possess good antimicrobial potential. Aims:: This study aimed to amalgamate sulfonamide, imidazole, and triazole moieties in a single molecular framework with the intent of improving their antimicrobial activities. Objective:: The objective of this study was the synthesis of conjugates containing sulfonamide and azole moieties along with in vitro and in silico evaluation as antimicrobial candidates. Method:: A series of sulfonamide-modified azoles (7a-r) was synthesized by multicomponent condensation of 1,2-dicarbonyl compounds, ammonium acetate and aryl-substituted aldehydes in glacial acetic acid. The structure of synthesized molecules was elucidated with the help of various spectroscopic techniques, such as FTIR, NMR, and HRMS. The target molecules were tested for in vitro antimicrobial potency against four bacterial strains and two fungal strains. Result:: Molecules 7c (MIC 0.0188 μmol/mL), 7f (MIC 0.0170 μmol/mL) and 7i (MIC 0.0181 μmol/mL) were most active against S. aureus and C. albicans. Against E. coli, molecules 7d (MIC 0.0179 μmol/mL), 7f (MIC 0.0170 μmol/mL) and 7i (MIC 0.0181 μmol/mL) were found to be highly active. Moreover, the binding conformations were investigated by in-silico molecular docking, and QTAIM (Quantitative theory of atoms in the molecule) analysis was also performed. Molecular properties, such as the heat of formation, HOMO energy, LUMO energy and COSMO volume, were found to be in direct correlation with the antimicrobial potency of molecules 7c, 7f and 7i against S. aureus and C. albicans. Conclusion:: All the synthesized molecules were more potent than clinically approved sulfonamides, namely sulfadiazine and sulfabenzamide.
背景::磺酰胺、咪唑和三唑化学核具有良好的抗菌潜力。目的本研究旨在将磺酰胺、咪唑和三唑分子合并到一个分子框架中,以提高它们的抗菌活性。目标::本研究的目的是合成含有磺酰胺和唑分子的共轭物,并将其作为候选抗菌剂进行体外和硅学评估。方法:在冰醋酸中通过多组分缩合 1,2-二羰基化合物、醋酸铵和芳基取代醛,合成了一系列磺酰胺修饰的唑类化合物(7a-r)。利用傅立叶变换红外光谱、核磁共振和 HRMS 等多种光谱技术阐明了合成分子的结构。测试了目标分子对四种细菌菌株和两种真菌菌株的体外抗菌效力。结果::分子 7c(MIC 0.0188 μmol/mL)、7f(MIC 0.0170 μmol/mL)和 7i(MIC 0.0181 μmol/mL)对金黄色葡萄球菌和白色念珠菌最有效。分子 7d(MIC 0.0179 μmol/mL)、7f(MIC 0.0170 μmol/mL)和 7i(MIC 0.0181 μmol/mL)对大肠杆菌具有很高的活性。此外,还通过室内分子对接研究了结合构象,并进行了 QTAIM(分子中原子定量理论)分析。研究发现,分子特性,如形成热、HOMO 能、LUMO 能和 COSMO 容量,与分子 7c、7f 和 7i 对金黄色葡萄球菌和白僵菌的抗菌效力直接相关。结论所有合成的分子都比临床批准的磺胺类药物(即磺胺嘧啶和磺胺苯甲酰胺)更有效。
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引用次数: 0
Importance and Green Synthesis of Amines: A Review 胺的重要性和绿色合成:综述
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-03-14 DOI: 10.2174/0113852728296565240221082253
Ashok Raj Patel, Ishwar Patel, Subhash Banerjee
: Amines are “derivatives of ammonia” and important key intermediates for applications in the industrial, pharmaceutical, electronics, etc. They have been used to synthesize industrially important azo dyes, which are used to color various materials. Moreover, amine functionality is present in several important biological molecules. Biogenic amines are found in living organisms and play essential physiological functions in the body. They are prepared from the amination and transamination reaction of carbonyl compounds such as aldehydes and ketones and the decarboxylation reaction of amino acids. Thus, the various applications and requirements of essential amine scaffolds paid attention to researchers to develop novel synthetic protocols to synthesize these compounds. In organic chemistry, various methods synthesize amines; however, green synthetic methods have recently become a trend. By writing this review, our main focus was to provide a brief on the importance of some biogenic amines and the synthesis of both amines via green synthetic methods.
:胺是 "氨的衍生物",是工业、医药、电子等领域应用的重要关键中间体。它们已被用于合成工业上重要的偶氮染料,这种染料可为各种材料着色。此外,胺功能还存在于一些重要的生物分子中。生物胺存在于生物体内,在体内发挥着重要的生理功能。它们是由醛、酮等羰基化合物的胺化和反式胺化反应以及氨基酸的脱羧反应制备而成的。因此,基本胺支架的各种应用和需求引起了研究人员的关注,他们致力于开发新的合成方案来合成这些化合物。在有机化学中,合成胺的方法多种多样,但绿色合成方法近年来已成为一种趋势。我们撰写这篇综述的主要目的是简要介绍一些生物胺的重要性以及通过绿色合成方法合成这两种胺的方法。
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引用次数: 0
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