异斯特维醇衍生物的应用研究进展

异斯特维醇是由天然产物甜菊糖苷经酸解得到,其衍生物在生物活性方面的应用研究较多。本文对异斯特维醇衍生物在生物活性、催化剂、分子识别和超分子组装等领域的应用进行了综述。     

哒嗪类衍生物除草活性研究进展

哒嗪类衍生物因具有广谱生物活性而引起广泛的关注,它在新型高效农药创制中起着重要作用.按照结构进行分类,对近年来哒嗪衍生物在除草剂中的应用作了综述,并对它的发展前景作进一步展望.     

噻吩并[3,2-c]吡啶类衍生物的研究进展

噻吩并吡啶类衍生物是一类具有重要生理活性和药用价值的杂环化合物,结构上类似于喹啉与异喹啉。近年来,关于噻吩并[3,2-c]吡啶类衍生物的研究有诸多报道,在抗菌、抗肿瘤、抗抑郁以及抗血栓等方面均呈现出良好的药理活性,现对噻吩并[3,2-c]吡啶类衍生物的生物活性作系统性回顾,为新药研究提供参考。     

咪唑并[2,1-b]噻唑衍生物的合成及生物活性进展

根据环上取代基的不同咪唑并[2,1-b]噻唑衍生物具有多种多样的生物活性。通过对咪唑并[2,1-b]噻唑衍生物合成方法的不同进行分类,综述了近年来咪唑并[2,1-b]噻唑衍生物的合成及其生物活性,结果表明在咪唑并噻唑环上引入药理活性基团会增强其生物活性。咪唑并[2,1-b]噻唑环一般由Hanzstch方法合成,近年来也出现了一些新的合成方法,如Sonogashira、Suzuki反应和金属催化芳基化,对这些新方法合成咪唑并噻唑环及其衍生物也进行了综述。     

靛蓝的生物活性研究进展

靛蓝不仅是常用染料,也在医药等领域广泛应用。本文综述了靛蓝的生物活性,靛蓝具有抗紫外线、抗氧化、抗菌、抗炎、免疫抑制等作用。全面认识靛蓝的生物活性有利于相关产品的更好开发利用。     

具有生物活性不饱和酸及其衍生物研究进展

源自天然产物不饱和酸衍生物具有新颖的化学结构和多种生物活性。综述了近年来天然不饱和酸衍生物及仿生合成不饱和酸衍生物的研究进展,初步总结了它们的生物活性。     

哒嗪类衍生物杀菌活性研究进展

哒嗪类衍生物因具有广谱生物活性而引起广泛的关注,将不同基团引入到哒嗪结构中,能产生具有杀菌活性的哒嗪类衍生物,使其在新型高效农药创制中起着重要作用.按照结构进行分类,对近年来哒嗪类衍生物在杀菌剂中的应用做了综述,并对它的发展前景做进一步展望.     

靛红双腙类化合物生物活性的研究进展

靛红双腙类化合物是一种重要的靛红衍生物,具有多种生物活性。为了进一步研究靛红双腙类化合物的生物活性与其构效关系,近年来人们对其结构进行了大量的修饰和改造,合成了一些活性较强的化合物。对近年来靛红双腙类化合物的生物活性及构效关系研究进行了综述。     

具有农药活性的噻唑酰胺类衍生物评述

噻唑类衍生物因具有独特的生物活性而受到广泛的关注.本文重点综述了噻唑酰胺类衍生物在农药生物活性方面的研究进展,对其发展趋势以及前景进行了展望.     

异吲哚啉衍生物的合成及应用进展

作为一类结构特殊且具有多种用途的重要含氮杂环化合物,异吲哚啉衍生物在医药化工等行业发挥着重要作用,尤其在药物分子设计合成及染料领域有着重要的应用。近年来,异吲哚啉及其衍生物的合成得到了快速的发展,各种异吲哚啉衍生物被合成,尤其是多取代异吲哚啉衍生物的合成及活性研究得到了广泛的关注。本文综述了异吲哚啉衍生物的合成方法,并对其在医药和化工领域的应用进行了介绍。     

The Effects of Methoxylated Isoindigo on the Optical and Charge Transport Properties of the Corresponding Polymers

Although the effects of electron-deficient group substitution on isoindigo on the corresponding conjugated polymers are extensively studied, the modification of isoindigo core with electron-rich groups has not been investigated. It is envisioned that the introduction of the methoxy group on isoindigo will not only tune the highest occupied molecular orbital (HOMO) energy level of the corresponding polymers but also introduce O···S “conformation lock” to increase the coplanarity of the polymers, which should facilitate hole transport. Herein, the syntheses of two methoxylated isoindigos and the investigations on the charge transport behaviors of their copolymers with bisthiophene ( 2T ) and bisthiazole ( 2Tz ) are reported. It is found that the substitution positions have a drastic influence on the UV–vis absorption and electrochemical properties for both monomers and polymers. Theoretical calculations and single crystal structure analysis confirm the existence of O···S “conformation lock”, however, both methoxy substitutions also change the aggregation behaviors of the corresponding polymers to a mixed face-on/edge-on orientation which has an adverse effect for charge transport. Among the four polymers, the polymer of 5,5'-methoxylated isoindigo and 2T exhibit the best hole mobility of 1.9 × 10⁻¹ cm² V⁻¹ s⁻¹.     

Halogenation effect promoted low bandgap polymers based on asymmetric isoindigo unit with low energy loss

To optimize the energy levels of the structural framework of isoindigo polymers, a series of asymmetric isoindigo based low bandgap polymers with chlorine, fluorine and thiazole substituents was constructed and their optical, electrochemical and photovoltaic properties were comparatively evaluated for the impact of different substitutions. In comparison with the polymer based on 2,2'‐bithiophene and isoindigo unit (PTi) with non‐substituted bithiophene as the donor moiety, the highest occupied molecular orbital energy level for the newly synthesized polymers is significantly decreased, and in turn an improvement of the open‐circuit voltage (V_OC) is noted in the corresponding photovoltaic devices. More importantly, combined with a low bandgap of 1.32 eV, the energy losses (E_loss) could be reduced to 0.61 eV for polymer based on chlorinated 2,2'‐bithiophene and isoindigo unit (PCl). In addition, the halogen moieties are observed to be superior in device fabrication and give better values than the thiazole substituent. Both fluorinated and chlorinated polymer donors exhibited improved performance compared with the original polymer PTi. Consequently, this work not only presents the influence of different electron withdrawing substituents on the physicochemical and photovoltaic performance, but also backs the concept of how to reduce the energy loss via the heteroatom effect. © 2020 Society of Chemical Industry     

具有农药活性的噻唑类化合物的研究进展

噻唑类化合物因具有良好的生物活性得到广泛的关注.重点介绍了近5年具有农药活性的噻唑酰胺、噻唑(硫)醚(砜)、噻唑丙烯腈、噻唑胺和哌啶噻唑类化合物进展,并对其生物活性及创制经纬进行了概述.     

相转移催化法合成二芳基对苯双氧乙酰基二硫脲类衍生物

以苯二氧乙酸为原料，用相转移催化法合成了8个1，4－对苯双氧乙酰基双硫脲类化合物，用IR、^1HNMR及元素分析及其结构进行了表征，经初步生物活性测试发现其中大多数化合具有良好的植物生长调节活性。     

线粒体单链DNA结合蛋白1与恶性肿瘤相关性的研究进展

线粒体单链DNA结合蛋白1(single-strand DNA-binding protein 1,SSBP1)是一种存在于线粒体的蛋白,主要参与线粒体相关生物学活动,目前相关研究发现,其与恶性肿瘤发生发展、转移及侵袭相关。本文就SSBP1与线粒体及恶性肿瘤之间的生物相关性作一综述。     

香豆素衍生物合成研究进展

香豆素衍生物因具有重要的生物、光学活性而受到人们的普遍关注。概述了近年来香豆素衍生物的主要合成方法,为香豆素衍生物的合成研究提供依据。     

In Vitro Anti-Proliferative and Apoptotic Effects of Hydroxytyrosyl Oleate on SH-SY5Y Human Neuroblastoma Cells

The antitumor activity of polyphenols derived from extra virgin olive oil and, in particular the biological activity of HTyr, has been studied extensively. However, the use of HTyr as a therapeutic agent for clinical applications is limited by its low bioavailability and rapid excretion in humans. To overcome these limitations, several synthetic strategies have been optimized to prepare lipophenols and new compounds derived from HTyr to increase lipophilicity and bioavailability. One very promising ester is hydroxytyrosyl oleate (HTyr-OL) because the chemical structure of HTyr, which is responsible for several biological activities, is linked to the monounsaturated chain of oleic acid (OA), giving the compound high lipophilicity and thus bioavailability in the cellular environment. In this study, the in vitro cytotoxic, anti-proliferative, and apoptotic induction activities of HTyr-OL were evaluated against SH-SY5Y human neuroblastoma cells, and the effects were compared with those of HTyr and OA. The results showed that the biological activity of HTyr was maintained in HTyr-OL treatments at lower dosages. In addition, the shotgun proteomic approach was used to study HTyr-OL-treated and untreated neuroblastoma cells, revealing that the antioxidant, anti-proliferative and anti-inflammatory activities of HTyr-OL were observed in the unique proteins of the two groups of samples.     

Recent Developments on the Synthesis and Biological Activities of Fused Pyrimidinone Derivatives

Heterocyclic compounds constitute a unique class of organic compounds endowed with a wide range of synthetic and pharmaceutical applications. Pyrimidinones and their fused analogues have received focused attention in this regard, partly due to their mimicry of nucleobases which consequently forges their interesting medicinal properties. Over the years, the medicinal chemistry research community has experienced an upsurge in articles describing the exploration of these scaffolds to develop effective therapeutic agents. Several biological activities, including antimicrobial, antiviral, anticancer, antidiabetic, anti-inflammatory, anticonvulsive, and antihistaminic, have been well documented. This minireview presents a compendium of recent developments (2017–2020) focused on the synthesis and biological activities of fused pyrimidinones. The goal is to update medicinal chemists on the therapeutic relevance of fused pyrimidinones and the molecular architecture of clinic-worthy drug candidates. A brief account of the structure-activity relationships (SAR) revealed from different biological assays is also discussed.     

具有杀虫杀螨活性的吡唑类化合物的研究进展

吡唑类衍生物是一类具有良好生物活性的化合物。概述了近十几年来文献报道最多的几类吡唑类衍生物的杀虫杀螨活性以及它们的结构特点。研究表明,此类化合物具有广泛生物活性,开发吡唑类杀虫、杀螨剂具有良好的发展前景。     

Marine Omega-3 Phospholipids: Metabolism and Biological Activities

The biological activities of omega-3 fatty acids (n-3 FAs) have been under extensive study for several decades. However, not much attention has been paid to differences of dietary forms, such as triglycerides (TGs) versus ethyl esters or phospholipids (PLs). New innovative marine raw materials, like krill and fish by-products, present n-3 FAs mainly in the PL form. With their increasing availability, new evidence has emerged on n-3 PL biological activities and differences to n-3 TGs. In this review, we describe the recently discovered nutritional properties of n-3 PLs on different parameters of metabolic syndrome and highlight their different metabolic bioavailability in comparison to other dietary forms of n-3 FAs.