具有生物活性的喹啉类化合物的最新进展

喹啉类化合物具有优良的生物、生理活性. 在医疗保健和植物保护方面, 喹啉类化合物显示了广泛的应用和发展前景. 综述近几年来喹啉类化合物在医药和农药方面的研究最新进展.     

2-取代芳基苯并呋喃类化合物生物活性及合成研究进展

综述了近十几年来报道的具有良好生物活性的2-芳基苯并呋喃类化合物, 以及这一类化合物结构骨架的构建与合成方法.     

Uncommon Terpenoids from Salvia Species: Chemistry,Biosynthesis and Biological Activities

The search for new bioactive compounds from plant sources has been and continues to be one of the most important fields of research in drug discovery. However, Natural Products research has continuously evolved, and more and more has gained a multidisciplinary character. Despite new developments of methodologies and concepts, one intriguing aspect still persists, i.e., different species belonging to the same genus can produce different secondary metabolites, whereas taxonomically different genera can produce the same compounds. The genus Salvia L. (Family Lamiaceae) comprises myriad distinct medicinal herbs used in traditional medicine worldwide that show different pharmacological activities due to the presence of a variety of interesting specialized metabolites, including mono-, sesqui-, di-, sester-, tri-, tetra-, and higher terpenoids as well as phenylpropanoids, phenolic acid derivatives, lignans, flavonoids, and alkaloids. We herein summarize the research progress on some uncommon terpenoids, isolated from members of the genus Salvia, which are well recognized for their potential pharmacological activities. This review also provides a current knowledge on the biosynthesis and occurrence of some interesting phytochemicals from Salvia species, viz. C₂₃-terpenoids, sesterterpenoids (C₂₅), dammarane triterpenoids (C₃₀), and uncommon triterpenoids (C₂₀+C₁₀). The study was carried out by searching various scientific databases, including Elsevier, ACS publications, Taylor and Francis, Wiley Online Library, MDPI, Springer, Thieme, and ProQuest. Therefore, 106 uncommon terpenoids were identified and summarized. Some of these compounds possessed a variety of pharmacological properties, such as antibacterial, antiviral, antiparasitic, cytotoxic and tubulin tyrosine ligase inhibitory activities. Due to the lack of pharmacological information for the presented compounds gathered from previous studies, biological investigation of these compounds should be reinvestigated.     

α-氨基膦酸及其酯的合成及生物活性的研究进展

α-氨基膦酸及其衍生物已成为国内外关注的热点.作为天然氨基酸的类似物,在医药、农药中起到越来越重要的作用,综述了有关2-氨基膦酸及其酯的合成、生物活性研究方面的工作,并对它的发展趋势、应用前景作了进一步的展望.     

具有生理活性甾体腙类化合物的研究进展

按照取代基类型将甾体腙类化合物进行分类.主要概述了近六年来新合成及发现的甾体腙类化合物及其衍生物的生理活性及研究进展,并对此方面的发展趋势、应用前景作了展望.     

Recent Advances in the Chemistry and Biological Activity of 2,4-Azepandione Ring System

The focus of this review is on the structure, methods of syntheses, chemical reactivity, and biological activity of 2,4-azepandione and some derivatives. Some important fused-ring systems containing 2,4-azepandione moiety were also reviewed.     

Substituted Pyrazoles and Their Heteroannulated Analogs—Recent Syntheses and Biological Activities

Pyrazoles are considered privileged scaffolds in medicinal chemistry. Previous reviews have discussed the importance of pyrazoles and their biological activities; however, few have dealt with the chemistry and the biology of heteroannulated derivatives. Therefore, we focused our attention on recent topics, up until 2020, for the synthesis of pyrazoles, their heteroannulated derivatives, and their applications as biologically active moieties. Moreover, we focused on traditional procedures used in the synthesis of pyrazoles.     

Semisynthesis and Pesticidal Activities of Novel Cholesterol Ester Derivatives Containing Cinnamic Acid-like Fragments

Due to the extensive use of agrochemicals resulting in the emergence of pesticide resistance and ecological environment problems, the research and development of new alternatives for crop protection is highly desirable. In order to discover potent natural product-based insecticide candidates, a series of new cholesterol ester derivatives containing cinnamic acid-like fragments at the C-7 position were synthesized. Some derivatives showed potent pesticidal activities. Against Mythimna separata Walker, compounds 2a, Id, Ig, and IIg showed 2.1–2.4-fold growth-inhibitory activity of the precursor cholesterol. Against Plutella xylostella Linnaeus, compounds Ig, IIf, and IIi exhibited 1.9–2.1-fold insecticidal activity of cholesterol. These results will pave the way for the future synthesis of cholesterol-based derivatives as agrochemicals.     

砷、锑、铋配合物的生物活性

合成新型砷、锑、铋的生物无机配合物并研究其构效关系与生物活性的作用机理,对于丰富生物无机化学内容、开发新的抗菌药和治疗肿瘤的化学药物都具有重要的意义和价值。本文简要综述了近年来砷、锑、铋的配合物在抗癌抗菌抗肿瘤等生物活性方面的应用,并展望了在该领域的应用前景。     

喹啉酮类化合物的合成及抗HIV活性研究进展

4-喹啉酮及其衍生物具有良好的抗病毒及抑制HIV-1整合酶活性。喹啉酮类化合物的合成研究成为抗HIV整合酶抑制剂研究开发的重要领域之一。文章着重从环合形成喹啉酮骨架的角度出发,综述了喹啉酮类化合物合成的最新进展,同时对其抗HIV活性作了简要介绍。     

酰基硫脲衍生物的合成、结构表征及生物活性研究

在超声波辐射下, 以PEG-400为固-液相转移催化剂, 用芳胺与双酰基异硫氰酸酯反应, 合成出了15种新的结构不对称的双酰基硫脲类化合物(6和6')和9种新的分子中含酰胺基团的单酰基硫脲类化合物(7和7'). 利用元素分析, IR, ¹H NMR, ¹³C NMR, APT, 1D NOE及2D NMR技术确定了所合成化合物6和6'及7和7'的结构, 并对它们NMR谱中低场C, H进行了归属. 杀菌、杀虫和除草活性筛选测定实验结果表明, 所测试化合物对瓜炭疽病菌均具有抑制作用, 其中6e抑制率最高, 达到62.4%; 目标化合物7a对黄瓜白粉病菌有一定的抑制作用. 单胺氧化酶活性测定实验表明：大部分目标化合物对单胺氧化酶具有一定的抑制活性, 其中浓度在1×10^－3 mol•L^－1时目标化合物6'c和6'd的抑制活性较强, 明显高于其它化合物. 目标化合物没有抗惊厥活性.     

Recent Advances in Excimer-Based Fluorescence Probes for Biological Applications

The fluorescent probe is a powerful tool for biological sensing and optical imaging, which can directly display analytes at the molecular level. It provides not only direct visualization of biological structures and processes, but also the capability of drug delivery systems regarding the target therapy. Conventional fluorescent probes are mainly based on monomer emission which has two distinguishing shortcomings in practice: small Stokes shifts and short lifetimes. Compared with monomer-based emission, excimer-based fluorescent probes have large Stokes shifts and long lifetimes which benefit biological applications. Recent progress in excimer-based fluorescent sensors (organic small molecules only) for biological applications are highlighted in this review, including materials and mechanisms as well as their representative applications. The progress suggests that excimer-based fluorescent probes have advantages and potential for bioanalytical applications.     

Synthesis, Characterization and Biological Activities of Novel Water-soluble Metalloporphyrins

Water-soluble metal porphyrins can sensitize photocatalytic water reduction1, oxidation2, and are of potential use in photogalvanic cells3. In recent years, porphyrins have been used as photosensitizer for the photodynamic therapy (PDT) of cancers. To constitute a good PDT photosensitizer, a compound must be soluble in the bodys tissue fluids so that it can be injected and carried around the body to the tumour site4. Research on the anti-tumor activity of metalloporphyrins has also been r…     

一对手性Salen型席夫碱对映体的合成、结构与生物活性

采取分步反应法以1R, 2R-环己二胺(或1S, 2S-环己二胺)先后与2-羟基萘甲醛和水杨酸苯酯反应, 合成了一对手性Salen型席夫碱对映体:1R-(2-羟基苯甲酰亚胺)-2R-(2-羟基萘甲亚胺)环己烷(1a)和1S-(2-羟基苯甲酰亚胺)-2S-(2-羟基萘甲亚胺)环己烷(1b), 对其进行了单晶结构、圆二色光谱、元素分析、红外光谱表征及生物活性实验。单晶结构与圆二色光谱分析表明1a和1b互为对映体;生物活性实验显示1a具有一定的抑菌活性。     

一对手性Salen型席夫碱对映体的合成、结构与生物活性

采取分步反应法以1R,2R-环己二胺(或1S,2S-环己二胺)与2-羟基萘甲醛和水杨酸苯酯反应,合成了一对手性Salen型席夫碱对映体:1R-(2-羟基苯甲酰亚胺)-2R-(2-羟基萘甲亚胺)环己烷(1a)和1S-(2-羟基苯甲酰亚胺)-2S-(2-羟基萘甲亚胺)环己烷(1b),对其进行了单晶结构、圆二色光谱、元素分析、红外光谱表征及生物活性实验。单晶结构与圆二色光谱分析表明1a和1b互为对映体;生物活性实验显示1a具有一定的抑菌活性。     

硫脲化合物的合成及其生物活性

硫脲化合物的合成及其生物活性董燕红，司宗兴（北京农业大学应用化学系北京１０００９４）关键词噻二陛－甲酰基，硫脲，胺类，合成，生物活性酰基硫脲在抗真菌、抗结核、抗病毒、除草以及调节植物生长方面具有广泛应用［１，２］。１，２，３－噻二唑杂环作为有效前体正...     

三氮杂大环及其衍生物的合成与其生物活性

合成了一种新的1,4,7-三氮杂十环配体及其4种衍生物,通过元素分析,IR,1HNMR和MS光谱对其结构进行了表怔。用人癌细胞Hela 和 HCT26对合成的目标化合物进行了生物活性研究,结果表明,所合成的化合物都有一定的抗肿瘤活性,并呈剂量效应关系,其中化合物4作用后的HCT26细胞呈现变性坏死的形态学改变,可明显诱导HCT26肿瘤细胞凋亡。     

糖苷化的亚氨基糖:分离、合成与生物活性

本文系统总结了糖苷化亚氨基糖的分离、合成方法与生物活性。天然存在的糖苷化的亚氨基糖根据其亚氨基糖部分的结构可以分为五类,大部分均具有重要的生物活性,尤其是糖苷酶抑制活性。此类化合物潜在的药理活性促进了相关合成方法的研究,根据糖苷键的构建方式大致可以分为酶催化的转糖基化反应和化学合成法,两者主要区别在于反应条件。酶催化的转糖基化反应条件温和,且能够减少保护基的使用,但在反应效率和选择性上仍需改进。化学合成法普适性高,有大量普通糖苷的合成经验可供借鉴,但存在反复上保护-脱保护的问题。通过以上两种合成方法,大量衍生物和类似物被设计和合成出来,大大丰富了糖苷化亚氨基糖的种类和生物活性。糖苷化亚氨基糖的生物活性往往与糖基结构和亚氨基糖环均有密切关系。作为传统糖化学与亚氨基糖的交叉领域,糖苷化亚氨基糖的结构多样性为发展高活性和选择性的先导化合物提供了优良的修饰骨架。因此,此类化合物有望在相关新药创制领域得到重要应用。     

具有生理活性的含氧、氮、硫杂原子螺环化合物的研究进展

综述了近年来部分具有生理活性螺环化合物的研究进展, 重点介绍了这类化合物的结构特征、生理活性和部分化合物的合成方法. 展望了该类螺环化合物的应用前景.     

新型汉防己甲素衍生物的合成及其生物活性

以汉防己甲素为原料,经溴代反应制得关键中间体5-溴汉防己甲素(2); 2与硼酸衍生物经Suzuki反应合成了6个新型的汉防己甲素衍生物(4a~4f),其结构经¹H NMR, ¹³C NMR和ESI-MS表征。采用CCK-8法初步考察了4a~4f对人早幼粒白血病细胞(HL60)和人肺癌细胞(A549)的抑制活性;并采用MTT法对活性较好的化合物进行复筛。采用酶联免疫吸附法考察4a~4f对多种受体酪氨酸激酶的抑制活性。结果表明：4b, 4c和4e对HL60和A549有一定的抑制活性; 4b和4c对受体酪氨酸激酶FGFR1的抑制活性大于50%。