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Anti-inflammatory alkaloids targeting IL-1 against Respiratory Viral infections: A Special insight into drug development against SARS-CoV 2 靶向IL-1的抗炎生物碱对抗呼吸道病毒感染:对严重急性呼吸系统综合征冠状病毒2型药物开发的特别见解
IF 2.3 4区 化学 Q2 CHEMISTRY, ORGANIC Pub Date : 2023-08-21 DOI: 10.2174/1570193x20666230821143410
S. Batool, Laiba Asim, Jin Zhang, Fawad Raffaq Qureshi, R. Saleem
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is one of the deadliest viruses among respiratory viruses which resulted in COVID-19 pandemic. The virus gets transmitted by the nasal route and moves down to the trachea, bronchi, and then to the lungs. Once replicated inside the alveolar cells, the SARS-CoV-2 makes the membrane of the alveolar sac porous, which causes the leaking of plasma from surrounding blood vessels into the alveolar sac leading to its buildup. This process results in the production of pro-inflammatory cytokines like interleukin-1β (IL-1β) and Tumor necrosis factor-α (TNF-α) by the helper T-cells at the site of the infection, causing difficulty in breathing. Plant-based alkaloids can be promising to treat viral infections. Plants have contributed to drug development against viruses like Herpes simplex virus (HSV), Human immunodeficiency virus (HIV), Hepatitis B virus (HBV), and viruses that cause respiratory diseases in humans. Plant alkaloids, either in the form of extract, infusion, or powder, have shown potential in treating viral diseases mainly by targeting the replication of viruses. Alkaloids like Tetrandrine, Oxymatrine, and Berberine have been shown to have a positive role in mediating pro-inflammatory cytokines like IL-1. These alkaloids thus inactivate the nuclear factor kappa-B (NF-kB) pathway, inhibiting the expression of its targeted genes, IL-1β and TNF-α. This inactivation of NF-kB results in reduced levels of IL-1 and TNF-α, and consequently reduced inflammation, decreasing the stress on the immune cells and increasing the ability of the patient to fight the infection. Despite vaccine development for SARS-CoV-2, the virus is continuously evolving into new varieties, posing a threat to humans and it is necessary to develop effective drug discovery programs. Natural products can pave the way in this regard. This review can contribute towards safer drug development against SARS-CoV-2, combating the threat of the ever-emerging variants of this virus.
严重急性呼吸综合征冠状病毒2 (SARS-CoV-2)是导致COVID-19大流行的呼吸道病毒中最致命的病毒之一。病毒通过鼻腔传播,向下移动到气管、支气管,然后进入肺部。一旦在肺泡细胞内复制,SARS-CoV-2就会使肺泡囊的膜多孔,从而导致血浆从周围血管渗漏到肺泡囊中,导致肺泡囊积聚。这一过程导致感染部位的辅助t细胞产生促炎细胞因子,如白细胞介素-1β (IL-1β)和肿瘤坏死因子-α (TNF-α),导致呼吸困难。植物生物碱有望治疗病毒感染。植物对对抗单纯疱疹病毒(HSV)、人类免疫缺陷病毒(HIV)、乙型肝炎病毒(HBV)和导致人类呼吸道疾病的病毒等病毒的药物开发做出了贡献。植物生物碱主要通过靶向病毒的复制来治疗病毒性疾病,无论是提取物、输液还是粉末形式。生物碱如粉防己碱、氧化苦参碱和小檗碱已被证明在介导IL-1等促炎细胞因子方面具有积极作用。这些生物碱因此使核因子κ b (NF-kB)通路失活,抑制其靶基因IL-1β和TNF-α的表达。NF-kB的失活导致IL-1和TNF-α水平降低,从而减少炎症,减少免疫细胞的压力,提高患者抵抗感染的能力。尽管开发了针对SARS-CoV-2的疫苗,但该病毒不断演变成新品种,对人类构成威胁,因此有必要制定有效的药物开发计划。天然产品可以在这方面铺平道路。这一综述有助于开发针对SARS-CoV-2的更安全的药物,对抗这种病毒不断出现的变种的威胁。
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引用次数: 0
Recent Advances in Transition Metal Catalyzed Synthesis of C3-Substitution-free 2-Oxindole Derivatives 过渡金属催化合成无c3取代2-吲哚衍生物的研究进展
4区 化学 Q2 CHEMISTRY, ORGANIC Pub Date : 2023-08-21 DOI: 10.2174/1570193x20666230821102422
Debapratim Das, Partha Pratim Das
Abstract: 2-Oxindole unit is one of the most important scaffolds found in several alkaloids, natural products, antitumor agents, pharmaceutically important compounds, etc. Molecules containing the 2-oxindole moiety were first isolated from the cat claw plant, widely distributed in the Amazon jungle. It has now been demonstrated that these molecules are present in a wide range of chemicals derived from plant sources. The capacity of 2-oxindole to be altered by various chemical groups to provide unique biological activities can be attributed to its function as a chemical framework for creating and devel-oping biological medications. Since the development of its first synthetic methodology, several re-search groups have developed protocols for producing 2-oxindole core and its bioactive derivatives. These include the traditional method and the transition/non-transition metal-catalyzed pathway for the synthesis of C3-non-substituted/C3-mono-substituted/C3-di-substituted core. Among those, C3-substitution-free 2-oxindole core synthesis is quite a challenging task, as C3-centre is very reactive. Syntheses of C3-substitution-free 2-oxindole cores have been less explored compared to other substi-tuted 2-oxindole derivatives. In this review article, we have mainly focused on showcasing the transi-tion metal-catalyzed synthetic methodology for the synthesis of 2-oxindoles with no substitution at C3-centre.
摘要:2-吲哚基是生物碱、天然产物、抗肿瘤药物、重要药用化合物等中最重要的支架结构之一。含有2-吲哚部分的分子最初是从广泛分布于亚马逊丛林的猫爪植物中分离出来的。现在已经证明,这些分子存在于从植物来源提取的各种化学物质中。2-吲哚被各种化学基团改变以提供独特生物活性的能力可归因于其作为创建和开发生物药物的化学框架的功能。自从开发出第一种合成方法以来,几个研究小组已经开发出了生产2-氧吲哚核心及其生物活性衍生物的方案。包括合成c3 -非取代/ c3 -单取代/ c3 -双取代核心的传统方法和过渡/非过渡金属催化途径。其中,无c3取代的2-氧吲哚中心的合成是一个非常具有挑战性的任务,因为c3中心的反应性很强。与其他取代的2-氧吲哚衍生物相比,对无c3取代的2-氧吲哚核心的合成研究较少。在这篇综述文章中,我们主要展示了过渡金属催化合成在c3中心没有取代的2-氧吲哚的方法。
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引用次数: 0
Epigrammatic Review on Heterocyclic Moiety Pyrazole: Applications and Synthesis Routes 杂环基吡唑的应用及合成路线
IF 2.3 4区 化学 Q2 CHEMISTRY, ORGANIC Pub Date : 2023-08-15 DOI: 10.2174/1570193x20666230815143007
Sapna Jain
Heterocyclic compounds are amongst the most promising and versatile classes of biologically important molecules. One of the heterocycle molecules is pyrazole with a five-membered heterocyclic ring with two neighboring nitrogen. Pyrazole and its derivatives have shown a broad range of biological applications like antibacterial, antifungal, antiviral, anti-inflammatory, anti-cancerous, and herbicidal activities. The study of synthetic routes suggests three broad ways: cyclo-condensation of hydrazine and its derivatives on 1,3 difunctional systems, dipolar cycloadditions, and multicomponent reactions. The synthesis of pyrazoles involves the usage of a conventional catalyst and more progressive and efficient nanoparticles as catalysts. The use of nanocatalysts is grabbing the attention of researchers owing to their more efficacy and reproducibility, low cost, reusability, ease of production, etc. The current review is an epigrammatic study on the importance of pyrazole as a biologically important moiety, recent advances in the three aforementioned routes to synthesize pyrazole and its derivatives, and a brief on the importance of nanocatalysts.
杂环化合物是最有前途和用途最广泛的一类生物重要分子。杂环分子之一是吡唑,它具有一个五元杂环和两个相邻的氮。吡唑及其衍生物具有广泛的生物学应用,如抗菌、抗真菌、抗病毒、抗炎、抗癌和除草活性。合成路线的研究提出了三种广泛的途径:肼及其衍生物在1,3双官能体系上的环缩合、偶极环加成和多组分反应。吡唑的合成涉及使用常规催化剂和更进步和有效的纳米颗粒作为催化剂。纳米催化剂的使用因其更有效、更重复、成本低、可重复使用、易于生产等优点而吸引了研究人员的注意。本文综述了吡唑作为生物重要部分的重要性、上述三种合成吡唑及其衍生物途径的最新进展,并简要介绍了纳米催化剂的重要性。
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引用次数: 0
Meet the Editorial Board Member 与编辑委员会成员见面
IF 2.3 4区 化学 Q2 CHEMISTRY, ORGANIC Pub Date : 2023-08-01 DOI: 10.2174/1570193x2005230227103846
Basha R. Sidick
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引用次数: 0
Recent Advances in Total Synthesis of Tetrahydroisoquinoline Alkaloids Quinocarcin and Lemonomycin 四氢异喹啉类生物碱、喹诺卡因和柠檬霉素的全合成研究进展
IF 2.3 4区 化学 Q2 CHEMISTRY, ORGANIC Pub Date : 2023-08-01 DOI: 10.2174/1570193x20666230801101427
Yang Yang, Junan Guo, Lanhua Shen, Jingyi Li, Fuan Li, Sifan Wang
Tetrahydroisoquinoline natural products are a kind of alkaloids containing various pharmacological activities. These structurally diverse alkaloids mainly consist of two subclasses, monotetrahydroisoquinolines(MTHI) and bistetrahydroisoquinolines(BTHI). Since its family member, Ecteinascidin-743 (INN: Trabectedin, trade name: Yondelis® ), has been approved by European Union in 2007 and the FDA in 2015 for the treatment of advanced soft tissue tumors, the research on this kind of natural product is full of new vitality. Quinocarcin and lemonomycin share a common diazabicyclo[3.2.1]octane framework that belongs to the subclass of MTHI, and their excellent antitumor activity and challenging architecture have made them an ideal target for total synthesis. In this short review, the progress in the total synthesis of quinocarcin and lemonomycin is summarized.
四氢异喹啉天然产物是一类具有多种药理活性的生物碱。这些生物碱结构多样,主要包括单四氢异喹啉(MTHI)和双四氢异喹啉(BTHI)两个亚类。自家族成员Ecteinascidin-743 (INN: Trabectedin,商品名:Yondelis®)于2007年获欧盟批准,2015年获FDA批准用于晚期软组织肿瘤治疗以来,对这类天然产物的研究充满了新的活力。喹诺卡素和柠檬霉素具有共同的重氮比环[3.2.1]辛烷值框架,属于MTHI亚类,其优异的抗肿瘤活性和具有挑战性的结构使其成为全合成的理想靶点。本文综述了喹诺卡素和柠檬霉素全合成的研究进展。
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引用次数: 0
Hydrogen bonding in triflamide and its derivatives 三氟甲酰胺及其衍生物中的氢键
IF 2.3 4区 化学 Q2 CHEMISTRY, ORGANIC Pub Date : 2023-07-25 DOI: 10.2174/1570193x20666230725103217
I. Sterkhova, B. Shainyan
This review focuses on studying hydrogen bonds in triflamide derivatives, the supramolecular structures formed in a crystal, solution, and gas phase, and the relationship between structural, spectral data and quantum chemical calculation data.
这篇综述的重点是研究三氟甲酰胺衍生物中的氢键,在晶体、溶液和气相中形成的超分子结构,以及结构、光谱数据和量子化学计算数据之间的关系。
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引用次数: 0
Alkaloids and Polyketides from Mangrove Associated Fungi viz. Aspergillus sp. and Penicillium sp. and Fusarium sp.: A review 红树林伴生真菌曲霉、青霉和镰刀菌的生物碱和聚酮研究进展
IF 2.3 4区 化学 Q2 CHEMISTRY, ORGANIC Pub Date : 2023-07-18 DOI: 10.2174/1570193x20666230718115115
A. Fulke, Avinash Awashank, Supriya Tilvi
In-depth research is being carried out on mangrove communities, which are regarded as significant habitats for biodiversity, in order to find novel secondary metabolites with useful pharmaceutical and medicinal uses. According to a growing number of articles that point to the enormous potential of this ecological niche, mangrove-associated fungi are acknowledged as a rich source of bioactive chemicals. The fungi Aspergillus sp., Penicillium sp., and Fusarium sp., which are isolated from the plant's leaves, rhizosphere, rhizospheres’ soil, and pneumatophore, are mangrove-associated and derived, according to this review. The secondary metabolites produced by fungi originating from mangroves, including alkaloids and polyketides, are discussed in this research, along with how these fungi are the source of bioactive chemicals with potent bioactivities, including antibacterial, anti-inflammatory, antioxidant, antifungal, and anticancer properties.
目前正在对被视为生物多样性重要栖息地的红树林群落进行深入研究,以寻找具有有用药用价值的新型次级代谢产物。根据越来越多的文章指出这种生态位的巨大潜力,红树林相关真菌被认为是生物活性化学物质的丰富来源。根据这篇综述,从植物的叶子、根际、根际土壤和气孔菌中分离出的真菌曲霉属、青霉属和镰刀菌属与红树林相关并衍生。本研究讨论了红树林真菌产生的次生代谢产物,包括生物碱和聚酮,以及这些真菌如何成为具有强大生物活性的生物活性化学物质的来源,包括抗菌、抗炎、抗氧化、抗真菌和抗癌特性。
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引用次数: 0
Diverse Heterocyclic Molecules Targeting Oxidative Stress as Therapeutic Effects Against Various Neurological Diseases 靶向氧化应激的多种杂环分子对各种神经系统疾病的治疗作用
IF 2.3 4区 化学 Q2 CHEMISTRY, ORGANIC Pub Date : 2023-07-11 DOI: 10.2174/1570193x20666230711170721
M. Asif, Saad Alghamdi, Ahmed Kabrah, E. B. Khidir, Issa Saad Al-Moraya
Heterocyclic compounds are the most common and diverse group of organic substances. Heterocyclic compounds are rapidly increasing in number as a result of intensive synthetic research as well as their value in other synthetic procedures. More than 90% of medications contain heterocyclic rings, and a wide range of medicinal chemistry applications make use of these substances. There are always unique characteristics of an efficient approach for creating newly discovered heterocyclic compounds and their moieties. Due to their biological effects, including those that are anti-cancer, anti-inflammatory, anti-fungal, anti-allergic, antibacterial, antiviral, and anticonvulsant, heterocyclic compounds are crucial to medicinal chemistry. Today's world population is generally suffering from various neurodegenerative diseases. Out of that, the most prevailing disease is Alzheimer's. There are many causes of Alzheimer's disease-like acetylcholinesterase enzyme, tau protein, amyloid aggregation, oxidative stress, phosphodiesterase, and others. In these cases, oxidative stress plays a very important role in the progression of this disease. To combat this oxidative stress various antioxidant-derived drugs have been used but the problem is that Alzheimer's progression cannot be targeted with a single target drug because of the other factors that are involved in its progression. So to overcome that, a drug targeting multiple targets has been synthesized by using the antioxidant in previous reports. These drugs are more potent and efficacious than single-target drugs. This review focused on various multi-target ligands to target oxidative stress.
杂环化合物是最常见和最多样化的一组有机物质。由于深入的合成研究以及杂环化合物在其他合成过程中的价值,杂环化合物的数量正在迅速增加。90%以上的药物含有杂环,广泛的药物化学应用都利用了这些物质。创造新发现的杂环化合物及其部分的有效方法总是具有独特的特点。杂环化合物具有抗癌、抗炎、抗真菌、抗过敏、抗菌、抗病毒和抗惊厥等生物作用,对药物化学至关重要。当今世界的人口普遍患有各种神经退行性疾病。其中,最常见的疾病是阿尔茨海默氏症。阿尔茨海默病的病因有很多,如乙酰胆碱酯酶、tau蛋白、淀粉样蛋白聚集、氧化应激、磷酸二酯酶等。在这些情况下,氧化应激在这种疾病的进展中起着非常重要的作用。为了对抗这种氧化应激,已经使用了各种抗氧化剂衍生的药物,但问题是,阿尔茨海默病的进展不能用单一的靶向药物来靶向,因为它的进展涉及其他因素。因此,为了克服这一点,在以前的报道中,已经使用抗氧化剂合成了一种靶向多个靶点的药物。这些药物比单一靶点药物更有效。这篇综述的重点是针对氧化应激的各种多靶点配体。
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引用次数: 0
Diphenyl ethers: Isolation, Bioactivities and Biosynthesis 二苯醚类化合物的分离、生物活性和生物合成
IF 2.3 4区 化学 Q2 CHEMISTRY, ORGANIC Pub Date : 2023-07-07 DOI: 10.2174/1570193x20666230707140919
Ning Chen, Bing-jing Liu, Yuxin Wang, Chenxue Li, Jintong Zhao, Ting Li
Diphenyl ethers (DPEs) are mainly produced by microorganisms and plants. The chemical structure of DPEs is relatively simple, and all of these compounds have the structure of biphenyl ethers in their chemical structure, the difference being the difference in the substituents on the benzene ring. Several recent studies have shown antibacterial, antioxidant, antitumor, antitumor, antihemolytic, neuroprotective, and anti-Alzheimer effects. DPEs could be candidate compounds for the treatment of Alzheimer's disease, by inhibiting the aggregation of Aβ42. Many DPEs from natural products exhibit good biological activity and they play an important role in the control of microbial infections. Diphenyl ethers have a wide range of applications and research value in the fields of pesticides, pharmaceuticals, textiles, household products, and public health. In this paper, we review the research progress of diphenyl ethers isolated from marine and plant endophytic sources in recent years, including their biosynthesis, and lay the foundation for further utilization and development.
二苯醚主要由微生物和植物产生。dpe的化学结构比较简单,这些化合物在化学结构上都具有联苯醚的结构,区别在于苯环上取代基的不同。最近的几项研究显示了抗菌、抗氧化、抗肿瘤、抗溶血、神经保护和抗阿尔茨海默病的作用。DPEs可以通过抑制a - β42的聚集而成为治疗阿尔茨海默病的候选化合物。许多天然产物的dpe具有良好的生物活性,在控制微生物感染方面发挥着重要作用。二苯醚在农药、医药、纺织、家居用品、公共卫生等领域有着广泛的应用和研究价值。本文综述了近年来从海洋和植物内生源分离的二苯醚及其生物合成的研究进展,为进一步利用和开发二苯醚奠定基础。
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引用次数: 0
Recent Progress in Synthetic Chemistry and Biological Activities of Pyrimido[4,5-b] Quinoline Derivatives (part III) 嘧啶并[4,5-b]喹啉衍生物的合成化学和生物活性研究进展(Ⅲ)
IF 2.3 4区 化学 Q2 CHEMISTRY, ORGANIC Pub Date : 2023-06-26 DOI: 10.2174/1570193x20666230626101436
M. Gouda, A. Abu‐Hashem, T. A. Ameen, M. A. Salem, Ateyatallah Aljuhan
Amongst heterocyclic compounds, quinoline and pyrimidine are advantaged scaffolds that appear as significant assembly motifs for the development of new drug entities. Moreover, quinoline-pyrimidine-inspired hybrids have a number of biological characteristics that are known. In addition, many pyrimido[4,5-b]quinoline ring systems (PyQs4,5-b), specifically concerning medicinal chemistry, have been reported over the past decade. The synthesis of (PyQs4,5-b) using barbituric acid, thiobarbituric acid, pyrimidine, and their derivatives is presented in this review. The preparation of PyQs4,5-b was clarified through the following chemical reactions: Friedländer, Vilsmeier-Haack formylation, Hantzsch-like reaction, and one-pot three-component reaction.
在杂环化合物中,喹啉和嘧啶是有利的支架,它们是开发新药实体的重要组装基序。此外,喹啉嘧啶激发的杂化物具有许多已知的生物学特性。此外,在过去的十年中,已经报道了许多嘧啶并[4,5-b]喹啉环系统(PyQs4,5-b),特别是关于药物化学。本文介绍了用巴比妥酸、硫代巴比妥酸、嘧啶及其衍生物合成(PyQs4,5-b)的方法。PyQs4,5-b的制备通过以下化学反应进行了澄清:Friedländer、Vilsmeier Haack甲酰化、类Hantzsch反应和一锅三组分反应。
{"title":"Recent Progress in Synthetic Chemistry and Biological Activities of Pyrimido[4,5-b] Quinoline Derivatives (part III)","authors":"M. Gouda, A. Abu‐Hashem, T. A. Ameen, M. A. Salem, Ateyatallah Aljuhan","doi":"10.2174/1570193x20666230626101436","DOIUrl":"https://doi.org/10.2174/1570193x20666230626101436","url":null,"abstract":"\u0000\u0000Amongst heterocyclic compounds, quinoline and pyrimidine are advantaged scaffolds that appear as significant assembly motifs for the development of new drug entities. Moreover, quinoline-pyrimidine-inspired hybrids have a number of biological characteristics that are known. In addition, many pyrimido[4,5-b]quinoline ring systems (PyQs4,5-b), specifically concerning medicinal chemistry, have been reported over the past decade. The synthesis of (PyQs4,5-b) using barbituric acid, thiobarbituric acid, pyrimidine, and their derivatives is presented in this review. The preparation of PyQs4,5-b was clarified through the following chemical reactions: Friedländer, Vilsmeier-Haack formylation, Hantzsch-like reaction, and one-pot three-component reaction.\u0000","PeriodicalId":18632,"journal":{"name":"Mini-reviews in Organic Chemistry","volume":" ","pages":""},"PeriodicalIF":2.3,"publicationDate":"2023-06-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48386354","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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Mini-reviews in Organic Chemistry
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