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Organophosphorus Synthesis beyond P-Cl Bond: The Development of Shelf-stable Reagents for [RP] Transfer 超越 P-Cl 键的有机磷合成:开发用于 [RP] 转移的货架稳定试剂
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-06-26 DOI: 10.2174/0113852728323258240613061150
Vadim D. Romanenko
: The direct chlorine-free incorporation of P1 units into organic molecules has very important synthetical value owing to environmental considerations and the prospect of accessing unique compounds with fascinating structures and useful properties. This selective survey presents a panorama of phosphorus species that are synthetic equivalents of free singlet phosphinidenes [R-P] and highlights the state-of-art of the [RP]- transfer reactions with emphasis on the synthesis of molecular architectures difficult to reach using traditional methods. Among stabilized phosphinidene precursors capable of RP-transfer are terminal transition-metal phosphinidene and phosphinidenoid complexes, dibenzo-7λ3 -phosphinobornadienes, phosphinidenephosphoranes, inversely polarized phosphaalkenes, phosphaketenes, intramolecularly base-stabilized phosphinidenes, (cyclo)polyphosphines and diphosphenes
:出于对环境的考虑,以及获得具有迷人结构和有用性质的独特化合物的前景,将 P1 单元直接无氯并入有机分子具有非常重要的合成价值。本研究选择性地介绍了作为游离单亚磷酸[R-P]合成等价物的磷物种的全景,并着重介绍了[RP]-转移反应的最新进展,重点是用传统方法难以合成的分子结构。能够进行 RP 转化的稳定亚膦烯前体包括末端过渡金属亚膦烯和亚膦烯类配合物、二苯并-7λ3 -亚膦硼烷、亚膦烯磷烷、反极化亚膦烯、亚膦烯、分子内碱稳定亚膦烯、(环)多膦和二磷酸盐。
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引用次数: 0
Advancements in the Synthesis of Triazolopyrimidines 三唑并嘧啶的合成进展
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-06-26 DOI: 10.2174/0113852728313437240607095009
Sushma Singh, Raman Lakhia, Sidhant Yadav, Poonam Devi, Karmvati Yadav, Vishwas Chaudhri, Rashmi Pundeer
: The triazolopyrimidine scaffold indeed holds a prominent place in medicinal chemistry due to its versatile pharmacological properties. Researchers have explored the scaffold and its derivatives for various therapeutic applications. The unique structure of triazolopyrimidine has made it a valuable template for designing medicinally active molecules. The literature is full of studies showcasing the synthesis and biological activities of compounds containing the triazolopyrimidine ring, either fused or coupled with other heterocycles. The aim of this review is to provide a comprehensive and general summary of the recent advancements in the synthesis of triazolopyrimidine derivatives (Year 2021 to present).
:三唑并嘧啶支架因其多变的药理特性而在药物化学中占有重要地位。研究人员已经探索了该支架及其衍生物在各种治疗中的应用。三唑并嘧啶的独特结构使其成为设计药用活性分子的宝贵模板。大量文献研究展示了含有三唑并嘧啶环(与其他杂环融合或偶联)的化合物的合成和生物活性。本综述旨在对三唑并嘧啶衍生物合成方面的最新进展(2021 年至今)进行全面而概括的总结。
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引用次数: 0
Chitosan/Bioglass Nanocomposites for Bone Tissue Engineering and Regenerative Medicine: An Overview of Promising Biomaterials 壳聚糖/生物玻璃纳米复合材料用于骨组织工程和再生医学:前景广阔的生物材料概述
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-06-26 DOI: 10.2174/0113852728314706240529052535
Khashayar Khodaverdi, Seyed Morteza Naghib, M.R. Mozafari
: Bioactive glass (BG) shows great potential as a biomaterial for bone regeneration. Chitosan enhances the biological characteristics of BG. Chitosan is the sole commonly utilized natural polysaccharide that may be chemically altered for various purposes and roles. Composite materials formed by combining chitosan bioactive glass (BG) nanoparticles and microparticles are used in this context. Integrating bioactive glasses enhances the mechanical characteristics, bioactivity, and regenerative capacity of the end product. Research indicates that chitosan/BG composites enhance angiogenesis, cell adhesion, and proliferation. Bioglass improves biomineralization and boosts bone extracellular matrix formation by osteoblasts. The current findings demonstrate that the chitosan-glass nanofiber composites can enhance both antibacterial capabilities and bone conductivity. This review examines novel techniques for creating chitosan-based materials for engineering purposes, as well as upcoming difficulties and outlooks.
:生物活性玻璃(BG)作为骨再生生物材料具有巨大潜力。壳聚糖增强了生物活性玻璃的生物特性。壳聚糖是唯一常用的天然多糖,可通过化学变化达到各种目的和作用。壳聚糖生物活性玻璃(BG)纳米颗粒和微颗粒形成的复合材料被应用于这一领域。结合生物活性玻璃可增强最终产品的机械特性、生物活性和再生能力。研究表明,壳聚糖/BG 复合材料可促进血管生成、细胞粘附和增殖。生物玻璃可改善生物矿化,促进成骨细胞形成细胞外基质。目前的研究结果表明,壳聚糖-玻璃纳米纤维复合材料可增强抗菌能力和骨传导性。本综述探讨了创建壳聚糖基工程材料的新技术,以及即将面临的困难和前景。
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引用次数: 0
Bio-Printing of Materials for Bone Tissue Engineering 用于骨组织工程的生物打印材料
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-06-24 DOI: 10.2174/0113852728312464240529050217
Taha Jafari, Seyed Morteza Naghib, M.R. Mozafari
: The complicated internal mechanical and structural qualities of normal bone tissue still prevent the development of effective therapeutic procedures for major bone lesions. It is still difficult to use tissue engineering to return damaged bones back to how they were originally intended. Due to recent advances in 3D printing, together with the introduction of new materials and technological assistance, the basis for BTE has been established. Biological 3D biomaterials have cells inside them, which allows for the creation of structures that mimic real tissues. Microextrusion, inkjet, and laser-assisted bioprinting are the three primary methods used in 3D bioprinting manufacturing. Hydrogels packed with cells, growth hormones, and bioactive ceramics are among the bioinks utilized in bone bioprinting. With the use of magnetic resonance imaging or computed tomography scanning, 3D printing offers substantial benefits for tailored treatment by enabling the creation of scaffolds with the right structural qualities, form, and dimensions. Three-dimensional (3D) bioprinting is a cutting-edge technique that has been utilized recently to create multicellular, biomimetic tissues with layers upon layers of intricate tissue microenvironment printing. We approached the use of hydrogels with great strength in 3D printing for BTE with an emphasis on first providing a thorough study about the development of 3D printing, printing techniques, and ink selection in this review. A brief prediction on how 3D printing would advance in the future was made.
:正常骨组织内部复杂的机械和结构特性仍然阻碍着针对重大骨损伤的有效治疗程序的开发。要利用组织工程学将受损骨骼恢复到原来的样子,仍有困难。由于三维打印技术的最新进展,加上新材料的引入和技术的辅助,BTE 的基础已经建立。生物三维生物材料内部有细胞,因此可以创建模仿真实组织的结构。微挤压、喷墨和激光辅助生物打印是三维生物打印制造的三种主要方法。骨生物打印中使用的生物材料包括含有细胞、生长激素和生物活性陶瓷的水凝胶。利用磁共振成像或计算机断层扫描技术,三维打印技术可以制造出具有适当结构质量、形状和尺寸的支架,从而为定制治疗带来巨大优势。三维(3D)生物打印是一种尖端技术,最近已被用于创建多细胞生物仿生组织,层层打印出错综复杂的组织微环境。我们在这篇综述中探讨了水凝胶在三维打印 BTE 中的应用,重点是首先对三维打印的发展、打印技术和油墨选择进行深入研究。我们还简要预测了未来 3D 打印技术的发展方向。
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引用次数: 0
In silico/vitro Study of Antibacterial Effects of Non-toxic Cinnamic Amidoesters on Artemia salina 无毒肉桂酰胺酯对盐藻类抗菌作用的硅学/体外研究
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-06-24 DOI: 10.2174/0113852728310711240525123954
Alexandre Almeida-Júnior, Helivaldo Diógenes da Silva Souza, Abraão Pinheiro de Sousa, Maria Vitória Oliveira Dantas, Fabio Correia Sampaio, Jose Alixandre de Sousa Luis, Valnês da Silva Rodrigues-Junior, José Maria Barbosa-Filho, Gabriela Fehn Fiss, Petrônio Filgueiras de Athayde-Filho
: According to the PLOS Neglected Tropical Diseases Journal, infection caused by the Gram-negative bacterium Escherichia coli is a neglected tropical disease. Staphylococcus aureus is the most dangerous Grampositive bacterium among staphylococcal bacteria. Moreover, resistance to Mycobacterium tuberculosis is an urgent public health issue. In this sense, cinnamic acid and acetamide derivatives have been used as strategic nuclei in the design of antimicrobial agents. With the aim of investigating whether antibacterial activity is improved with the junction of cinnamic and acetamide nuclei, cinnamic amidoesters were planned and evaluated as potential antibacterial agents. In silico (ADMET test and molecular docking) and in vitro (antibacterial and antituberculosis evaluation, and toxicity on Artemia salina larvae) studies were performed. Twelve cinnamic amidoesters were synthesized, which present positive characteristics for possible drug candidates, and showed subtle activity against E. coli, however, against S. aureus, unsubstituted and para-substituted compounds (R3 = H, Me, Cl, Br) showed significant activity, with MIC = 156.25-625 μg.mL-1. Only one para-substituted compound (R3 = Bu) showed discrete activity against M. tuberculosis, with MIC = 200 μM. For the most active compounds against S. aureus, the molecular docking study demonstrated affinity with the TtRNA enzyme, which plays a central role in the assembly of amino acids into polypeptide chains. The most active compounds against S. aureus and M. tuberculosis were non-toxic on A. salina, with LC50 > 1000 μg.mL-1. According to in silico/vitro studies, the non-toxic compound 5h (R3 = Cl) stands out as a potential antibacterial agent for further studies.
:据《PLOS 被忽视的热带病杂志》报道,革兰氏阴性大肠杆菌引起的感染是一种被忽视的热带病。金黄色葡萄球菌是葡萄球菌中最危险的革兰氏阳性菌。此外,结核分枝杆菌的抗药性也是一个紧迫的公共卫生问题。因此,肉桂酸和乙酰胺衍生物已被用作设计抗菌剂的战略核心。为了研究肉桂酸和乙酰胺核的结合是否能提高抗菌活性,我们计划将肉桂酸酰胺酯作为潜在的抗菌剂进行评估。研究人员进行了硅学(ADMET 试验和分子对接)和体外(抗菌和抗结核评估以及对盐水蒿幼虫的毒性)研究。合成的 12 个肉桂酰胺酯具有可能成为候选药物的积极特征,对大肠杆菌表现出微弱的活性,但对金黄色葡萄球菌,未取代和对位取代的化合物(R3 = H、Me、Cl、Br)表现出显著的活性,MIC = 156.25-625 μg.mL-1。只有一个对位取代化合物(R3 = Bu)对结核杆菌表现出不连续的活性,MIC = 200 μM。分子对接研究表明,对金黄色葡萄球菌最具活性的化合物与 TtRNA 酶具有亲和力,而 TtRNA 酶在氨基酸组装成多肽链的过程中起着核心作用。对金黄色葡萄球菌和结核杆菌最有效的化合物对盐水青蛙无毒,半数致死浓度为 1000 μg.mL-1。根据硅学/体外研究,无毒化合物 5h(R3 = Cl)是一种潜在的抗菌剂,值得进一步研究。
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引用次数: 0
Synthesis of Polynuclear Aromatic Hydrocarbons by Palladium-catalyzed C-H Bond Functionalization 通过钯催化 C-H 键官能化合成多核芳香烃
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-06-24 DOI: 10.2174/0113852728283702240605113835
Mitali Dewan, Sachinath Bera, Shubhankar Samanta, Debasish Kundu, Rathin Jana
: Nowadays palladium-catalyzed C–H bond activation is a useful approach for the synthetic transformation of organic compounds due to step economy, the use of non-prefunctionalized substrates and reduced chemical wastes. Among the various synthetic strategies, palladium catalyzed intra and inter-molecular C–H bond activation has recently drawn a lot of interest to synthesize the decorated π-conjugated polycyclic aromatic hydrocarbon. In this review, we have focused on recent progress along with previous strategies to synthesize various polynuclear aromatic hydrocarbons (PAHs) by the use of Pd-catalyzed C–H bond activation. We have also discussed the mechanistic details of the reaction intra and inter-molecular C–H bond activation.
:如今,钯催化 C-H 键活化是一种有用的有机化合物合成转化方法,它具有步骤经济、使用非预官能化底物和减少化学废物等优点。在各种合成策略中,钯催化分子内和分子间 C-H 键活化最近在合成装饰性 π 共轭多环芳烃方面引起了广泛关注。在本综述中,我们重点介绍了利用 Pd 催化 C-H 键活化合成各种多核芳烃 (PAH) 的最新进展和以往的策略。我们还讨论了分子内和分子间 C-H 键活化反应的机理细节。
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引用次数: 0
Synthesis and Biological Evaluation of Gastroprotective Polymer Conjugates of Aceclofenac 阿昔洛芬酸胃保护性聚合物共轭物的合成与生物学评价
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-06-24 DOI: 10.2174/0113852728301376240604052622
Monika Mishra, Viney Chawla, Pooja A. Chawla
: Nonsteroidal anti-inflammatory drugs account for a sizeable fraction of the drugs prescribed worldwide. If consumed for a long time, they can cause ulcers and life-threatening side effects. Since the acidic group present in NSAIDs is mainly responsible for these side effects, the scientists try to synthesize polymer drug conjugates that avoid these side effects but still retain the potency of the parent drug. Macromolecular drug conjugates of aceclofenac were prepared by employing pectin, β cyclodextrin, deacetylated chitin (chitosan) and albumin (egg and bovine serum). The prepared conjugates were characterized and tested for their antiinflammatory, antinociceptive and antiulcerogenic activity. Further experimentation was undertaken to analyze the behavior of compounds and their stability in hydrolytic conditions. Test compound A1, a pectin conjugate of aceclofenac, exhibited significant antinociceptive and anti-inflammatory activity with a significant decrease in ulcer index (4.45±0.24) as against aceclofenac (8.61±0.40) or vehicle (12.39±0.44) treated group. A novel and safer polymer drug conjugate of aceclofenac has been synthesized and evaluated.
:非甾体类消炎药占全球处方药的很大一部分。如果长期服用,它们会导致溃疡和危及生命的副作用。由于非甾体抗炎药中的酸性基团是造成这些副作用的主要原因,科学家们试图合成聚合物药物共轭物,以避免这些副作用,但仍保留母药的药效。研究人员利用果胶、β 环糊精、脱乙酰甲壳素(壳聚糖)和白蛋白(鸡蛋和牛血清)制备了醋氯芬酸的大分子药物共轭物。对制备的共轭物进行了表征,并测试了其抗炎、抗痛觉和抗溃疡活性。进一步的实验分析了化合物的行为及其在水解条件下的稳定性。试验化合物 A1 是醋氯芬酸的果胶共轭物,与醋氯芬酸(8.61±0.40)或载体(12.39±0.44)处理组相比,具有显著的抗痛觉和抗炎活性,溃疡指数(4.45±0.24)显著下降。我们合成并评估了一种新型、更安全的醋氯芬酸聚合物药物共轭物。
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引用次数: 0
Recent Innovations in Synthetic Methodologies and Patent Landscape of Quinoline Analogues: A Comprehensive Review 喹啉类似物合成方法的最新创新和专利格局:全面回顾
IF 2.6 3区 化学 Q3 CHEMISTRY, ORGANIC Pub Date : 2024-06-24 DOI: 10.2174/0113852728311152240529082035
Tanvi Rajiv Goel, Salahuddin, Kavita Rana, Avijit Mazumder, Rajnish Kumar, Mohamed Jawed Ahsan, Mohammad Sarafroz, Pankaj Tyagi, Saurabh Singh
Quinoline is a general group of heterocyclic compounds that have garnered much interest in medicinal chemistry and drug development due to their wide range of pharmacological effects. Pyridine ring fused with benzene defines the class of chemical compounds known as quinolines. Quinoline is a weak tertiary base, also known as 1-aza-naphthalene. Numerous patents have been filed for the synthesis of quinoline-based compounds, discussing about their derivatives and uses. Here, we have discussed the methods of quinoline synthesis, structural alterations, and patents showing its importance in various industries. Quinolines have been investigated as antimalarial substances, with substances, like quinine and chloroquine, serving as notable examples, and they have also been investigated to possess anti-inflammatory, anti-tumor, and CNS activity. The synthesis of quinoline is also subjected to several recognized procedures. The variations in the ring system and various synthetic approaches are the key highlights of the article, and it includes the various catalysts that could be recycled and reused by the assisted technique, which increases the yield and requires less time for the synthesis (ultrasound-promoted synthesis, one-pot reaction, and microwave and photocatalytic reactions). The development of synthetic procedures can help in the sustainable synthesis of quinoline derivatives.
喹啉是一类杂环化合物,因其广泛的药理作用而在药物化学和药物开发领域备受关注。吡啶环与苯的融合决定了这一类化合物被称为喹啉。喹啉是一种弱三级碱,也称为 1-氮杂萘。关于喹啉类化合物的合成以及其衍生物和用途,已经申请了大量专利。在此,我们讨论了喹啉的合成方法、结构变化以及显示其在各行业重要性的专利。喹啉类化合物曾被研究用作抗疟药物,如奎宁和氯喹,它们还被研究用于抗炎、抗肿瘤和中枢神经系统活性。喹啉的合成也有几种公认的程序。环系统的变化和各种合成方法是文章的主要亮点,其中还包括可通过辅助技术回收和重复使用的各种催化剂,这些催化剂可提高产量并缩短合成所需的时间(超声促进合成、一锅反应以及微波和光催化反应)。合成程序的开发有助于喹啉衍生物的可持续合成。
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引用次数: 0
1-Thiosugars: From Synthesis to Applications 1-Thiosugars:从合成到应用
IF 2.6 3区 化学 Q3 Chemistry Pub Date : 2024-06-14 DOI: 10.2174/0113852728314452240524112438
Surabhi Gupta, Charles Gauthier
1-Thiosugars and their glycosides play crucial roles in carbohydrate chemistry, primarily due to theirstability and potential for mimicking O-glycosides. The synthetic methodologies for thioglycosides pose ongoingchallenges. In recent years, researchers have shown a growing interest in exploring the applications of thiosugarsin various fields, including the development of natural product derivatives, oligo- and polysaccharidemimics, metallodrugs, and dendrimers. Numerous approaches and protocols have been devised for the synthesisof thiosugars. This review aims to comprehensively cover the efforts towards preparing thiosugars and theirapplication as synthetic precursors.
1 硫代糖及其糖苷在碳水化合物化学中发挥着至关重要的作用,这主要是由于它们具有模仿 O 型糖苷的易用性和潜力。硫代糖苷的合成方法一直是个难题。近年来,研究人员对探索硫代糖苷在各个领域的应用表现出越来越浓厚的兴趣,包括开发天然产物衍生物、寡糖和多糖仿生、金属药物和树枝状聚合物。硫代糖合成的方法和方案层出不穷。本综述旨在全面介绍硫代糖的制备及其作为合成前体的应用。
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引用次数: 0
1,4-Diazabicyclo[2.2.2]octane (DABCO) in Organic Synthesis and Catalysis: AQuinquennial Report (2019-to date) 有机合成和催化中的 1,4-二氮杂双环[2.2.2]辛烷 (DABCO):五年期报告(2019 年至今)
IF 2.6 3区 化学 Q3 Chemistry Pub Date : 2024-06-12 DOI: 10.2174/0113852728313865240528073519
Ravi Varala, Vittal Seema, Mohammed Mujahid Alam, Mohammed Amanullah, Beda Durga Prasad
DABCO is one of the more effective basic organocatalysts/reagents that can be used for a range oforganic transformations, including C-H functionalization, formation of hetero-hetero bonds, rearrangements, thesynthesis of heterocyclic compounds, cyclizations and annulations, other miscellaneous reactions. Thisquinquennial review aims to critically and perceptively address noteworthy contributions of non chiral catalystDABCO for regular organic transformations from 2019 onward. The key areas of attention were the advantagesand limits of the approach, in addition to the mechanistic pathway, which is required for a specific organictransformation to be performed effectively.
DABCO 是较为有效的基本有机催化剂/试剂之一,可用于一系列有机转化,包括 C-H 功能化、杂-杂键的形成、重排、杂环化合物的合成、环化和环化以及其他杂项反应。这篇五年一度的综述旨在批判性地、敏锐地探讨非手性催化剂DABCO自2019年以来在常规有机转化中做出的值得注意的贡献。重点关注的领域包括该方法的优势和局限,以及有效进行特定有机转化所需的机理途径。
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引用次数: 0
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Current Organic Chemistry
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