雷沙吉兰甲磺酸盐的合成工艺研究

目的 优化雷沙吉兰甲磺酸盐合成工艺。方法 1-茚酮经一锅法还原-胺化制得1-氨基茚满,然后与3-溴丙炔反应得N-炔丙基-1-氨基茚满,用L-酒石酸拆分得R-(+)-N-炔丙基-1-氨基茚满酒石酸盐,最后碱化、成盐得雷沙吉兰甲磺酸盐。结果 中间体及目标产物结构经¹H-NMR和MS确证结构,5步总收率达19.2%。结论 此路线原料易得,反应条件温和,操作简便,收率高,适于工业化生产。     

抗血吸虫药茚满酮类及萘满酮类化合物的合成

取代水杨酰胺类化合物(包括氯硝柳胺)对动物日本血吸虫病有预防和治疗作用。取代茚满类化合物的结构与取代水杨酰胺类有相似之处。据此,合成了各种取代茚满酮类化合物91个,有效者为23个,其中以化合物8,15(S 72059),18,30,76效果较显著。有效化合物均具有酮肟结构,其药效专属性较为明显。     

甲磺酸雷沙吉兰的合成工艺改进

本研究改进了甲磺酸雷沙吉兰(1)的合成工艺.用对甲苯磺酰氯(2)与炔丙醇(3)在二氯甲烷中反应得到对甲苯磺酸炔丙酯(4).另用1-茚酮(5)与甲酸铵、10％钯炭在常温常压下反应得到1-氨基茚满(6),与4反应得到N-炔丙基-1-氨基茚满(7),再经L-酒石酸拆分得到二[(R)-(+)-N-炔丙基-1-氨基茚]-L-酒石...     

天然来源的浅蓝霉素类化合物△*

浅蓝霉素类化合物是一类微生物产生的的生物碱,结构中大多含有1个2,2′-联吡啶母核。自从1959年发现首个浅蓝霉素类化合物（浅蓝霉素A）以来,共报道了49个天然来源的浅蓝霉素类化合物。由于2,2′-联吡啶和醛肟基团的存在,浅蓝霉素类化合物表现出抗菌活性、细胞毒活性、免疫调节等生物活性,一直是化学家、生物学家和药物学家重点关注的对象。本文综述了这49个天然来源的浅蓝霉素类化合物的结构与生物活性,旨在为该类化合物的深入研究提供有益的参考。     

海洋药物—生态功能及其应用于海洋生物药研究的展望

海洋存在大量的生物多样性品种,以往人类主要从海洋生物资源中获得蛋白质,近年来,天然产物化学家开始从大量的海洋无脊椎动物如海绵,被囊动物,苔藓虫类及其其它如海藻等发现生物活性次生代谢产物,多种该类化合物具有强生物活性如抗肿瘤并已应用于临床研究,部分化合物则具有保护植物,（如天然杀虫剂）和作为天然化妆品配方的功能,本报告将报道具有新药开发前景的海洋天然产物的发展动态。在海洋中,生物活性分子通常作为化学保护以对抗环境的不利因素如被鱼软体动物吞噬,或竞争生存空间,本文将讨论从海绵中分到的天然产物的对鱼类的强拒食活性,众所周知,海洋无脊椎动物通常于各种海洋微生物包括细胞菌,真菌或微藻共生,这些微生物可能存在于细胞外,细胞内或存在于宿主细胞的核内,从结构特征看,海洋微生物可能参加了海洋无脊椎动物的代谢过程,因此,海洋天然产物化学家开始热衷于微生物天然产物－新药研究先导化合物的新资源的研究。     

环肽类化合物的合成与生物活性研究进展

对近年来在环肽化合物的化学合成和生物活性等方面的研究进展及该类化合物潜在的临床应用前景作一综述。环肽类化合物是一类结构新颖、生物活性广泛、作用机制独特的化合物,在天然产物中占据十分重要的地位,环肽的研究正在受到人们越来越多的关注。     

五环胍类生物碱的结构、合成及生物活性

五元胍类生物碱是目前分离得到的结构最为复杂的胍类生物碱.该类化合物由于具有独特的结构、优良的理化性质和多样的生物活性,引起了科学家的极大兴趣.本文将重点介绍此类天然产物的合成方法及其生物活性,以期为今后设计合成此类活性化合物指明方向.     

若干莽草酸衍生物的合成和生物活性研究

虽然对莽草酸(shikimic acid)的研究由来已久,但只是在陆续发现了具有生物活性的乙二醛酶Ⅰ抑制剂(glyoxalase Ⅰinhibitor 1)和二(口恶)霉素(dioxolamycin 2)等含莽草酸类母核的天然产物后,才有合成莽草酸衍生物进行生物活性研究的报道,即由莽草酸甲酯合成乙二醛酶Ⅰ抑制剂的类似物3。     

链霉菌属微生物来源的生物活性天然产物

链霉菌属微生物可合成结构多样且具有多种生物活性的天然产物,如抗微生物、抗肿瘤、酶抑制等。本文就近年来从链霉菌属微生物中分离得到的生物活性天然产物进行综述。     

含APD环缩酚酸肽类天然产物的研究进展

含有4-氨基-2,4-戊二烯酸的环缩酚酸肽类天然产物是一类包含酯键的环状多肽次级代谢产物,通常具有抗肿瘤、抗病原体等生物活性。此文根据国内外最新研究现状,介绍了这类物质的来源、结构、制备现状、生物活性以及开发前景。     

Naturally occurring phenylethanoid glycosides: potential leads for new therapeutics

Natural products have long been regarded as excellent sources for drug discovery given their structure diversity and wide variety of biological activities. Phenylethanoid glycosides are naturally occurring compounds of plant origin and are structurally characterized with a hydroxyphenylethyl moiety to which a glucopyranose is linked through a glycosidic bond. To date several hundred compounds of this type have been isolated from medicinal plants and further pharmacological studies in vitro or in vivo have shown that these compounds possess a broad array of biological activities including antibacterial, antitumor, antiviral, anti-inflammatory, neuro-protective, antioxidant, hepatoprotective, immunomodulatory, and tyrosinase inhibitory actions. Given their extensive activity profile, structure-activity relationships analyses of these compounds have been performed in a number of studies to reveal potential leads for future drug design. This article will summarize the major developments in phenylethanoid glycosides-based research in the past decade. The progresses made in phytochemistry and biological activity studies of these compounds will be reviewed. Particular attention will be given to the novel structures identified to date and the prominent therapeutic values associated with these molecules.     

香豆素类化合物的药理研究进展

通过查阅相关文献,对香豆素类化合物药理作用的研究现状进行综述。香豆素类化合物具有镇痛抗炎、抗艾滋病、抗肿瘤、抗氧化、降压、抗心律失常等多方面的生物活性,为香豆素类化合物的深入研究提供参考。     

Biomedical research tools from the seabed

This review covers the applications of small-molecule and peptidic compounds isolated from marine organisms for biomedical research. Enzymes and proteins from marine sources are already on the market for biomedical applications, but the use of small-molecule biomedical research tools of marine origin is less developed. For many studies involving these molecules the ultimate goal is the application of small-molecule therapeutics in the clinic, but those that do not succeed in the clinic still have clearly defined biological activities, which may be of use as biomedical research tools. In other cases, the investigation of marine-derived compounds has led directly to the discovery of therapeutics with clinical applications. Both as tools and therapeutics, these small-molecule compounds are effective for investigating biological processes, and in this review the authors have chosen to concentrate on the ability of marine natural products to affect membrane processes, ion channels and intracellular processes.     

查尔酮类化合物生物活性研究进展

查尔酮类化合物以1,3-二苯基丙烯酮为基本骨架结构,为多种药用植物的有效成分,具有广泛的生物学活性,因此人们对此类化合物进行了大量研究。了解该类化合物的药理作用机制和构效关系,可为新药设计和开发提供先导化合物或药物资源。现对查尔酮类化合物的抗肿瘤、抗寄生虫、抗HIV、抗炎等多种生物学活性的药理作用机制及构效关系进行了综述。     

环烯醚萜类化合物近年研究进展

目的 介绍环烯醚萜类化合物研究概况和近年研究进展。方法 以近年来国内外发表的文献为依据,从结构分类、半合成及生物活性方面综述环烯醚萜类化合物近年研究进展。结果 环烯醚萜类化合物具有多种生物活性。结论 环烯醚萜是一类很有研究价值的化合物。     

Acanthella属海绵化学成分及生物活性的研究进展

目的对Acanthella属海绵的化学成分及其生物活性进行综述。方法通过综述国内外相关文献,归纳总结了该属海绵的研究概况。结果从该属海绵中已分离鉴定110个化合物,主要为含有异腈基、异硫氰酸酯和甲酰胺等含氮基团的倍半萜、二萜类化合物。这类化合物具有抗疟、抗虫、抗污损、抗肿瘤、抗菌等多样的生物活性。结论为Acanthella属海绵的化学成分及生物活性的进一步研究提供依据。     

环烯醚萜类化合物的结构和生物学活性研究进展

目的：详细综述了新发现的、具有较新结构特点的环烯醚萜类化合物及生物学活性研究,为环烯醚萜类化合物的结构活性研究提供新的思路。方法：查阅总结近30年国内外发表的关于环烯醚萜新化合物的文献,总结结构和活性的研究概况。结果：环烯醚萜的主要结构类型环烯醚萜苷类、裂环环烯醚萜和环烯醚萜酯。环烯醚萜类化合物主要临床生物活性具有神经系统的保护作用、抗肿瘤作用和保肝作用等。结论：环烯醚萜类化合物的分布广泛,具有较大的药用价值。通过对环烯醚萜类化合物结构和生物学活性的总结和分析,探讨环烯醚萜化合物结构与活性之间的关系,为药物开发和利用提供文献和数据支持。     

Recent cancer drug development with xanthone structures

Objectives Xanthones are simple three‐membered ring compounds that are mainly found as secondary metabolites in higher plants and microorganisms. Xanthones have very diverse biological profiles, including antihypertensive, antioxidative, antithrombotic and anticancer activity, depending on their diverse structures, which are modified by substituents on the ring system. Although several reviews have already been published on xanthone compounds, few of them have focused on the anticancer activity of xanthone derivatives. In this review we briefly summarize natural and synthetic xanthone compounds which have potential as anticancer drugs. Key findings The interesting structural scaffold and pharmacological importance of xanthone derivatives have led many scientists to isolate or synthesize these compounds as novel drug candidates. In the past, extensive research has been conducted to obtain xanthone derivatives from natural resources as well as through synthetic chemistry. Xanthones interact with various pharmacological targets based on the different substituents on the core ring. The anticancer activities of xanthones are also dramatically altered by the ring substituents and their positions. Summary The biological activities of synthetic xanthone derivatives depend on the various substituents and their position. Study of the biological mechanism of action of xanthone analogues, however, has not been conducted extensively compared to the diversity of xanthone compounds. Elucidation of the exact biological target of xanthone compounds will provide better opportunities for these compounds to be developed as potent anticancer drugs. At the same time, modification of natural xanthone derivatives aimed at specific targets is capable of expanding the biological spectrum of xanthone compounds.     

Recent researches in triazole compounds as medicinal drugs

Triazole compounds containing three nitrogen atoms in the five-membered aromatic azole ring are readily able to bind with a variety of enzymes and receptors in biological system via diverse non-covalent interactions, and thus display versatile biological activities. The related researches in triazole-based derivatives as medicinal drugs have been an extremely active topic, and numerous excellent achievements have been acquired. Noticeably, a large number of triazole compounds as clinical drugs or candidates have been frequently employed for the treatment of various types of diseases, which have shown their large development value and wide potential as medicinal agents. This work systematically reviewed the recent researches and developments of the whole range of triazole compounds as medicinal drugs, including antifungal, anticancer, antibacterial, antitubercular, antiviral, anti-inflammatory and analgesic, anticonvulsant, antiparasitic, antidiabetic, anti-obesitic, antihistaminic, anti-neuropathic, antihypertensive as well as other biological activities. The perspectives of the foreseeable future in the research and development of triazole-based compounds as medicinal drugs are also presented. It is hoped that this review will serve as a stimulant for new thoughts in the quest for rational designs of more active and less toxic triazole medicinal drugs.     

Rhodanine as a scaffold in drug discovery: a critical review of its biological activities and mechanisms of target modulation

INTRODUCTION: Rhodanine-based compounds have been associated with numerous biological activities. After many years of research in drug discovery, they have gained a reputation as being pan assay interference compounds (PAINS) and frequent hitters in screening campaigns. Rhodanine-based compounds are also aggregators that can non-specifically interact with target proteins as well as Michael acceptors and interfere photometrically in biological assays due to their color. AREAS COVERED: The authors review the recently reported biological activities of rhodanine-based compounds. Furthermore, the article provides details of their synthesis and occurrence in compound libraries through high-throughput screening (HTS) and virtual high-throughput screening (VHTS). Additionally, the authors provide the reader with possible mechanisms of non-specific target modulation, analysis of the crystal structures of enzyme-rhodanine complexes and a comparison of rhodanine and thiazolidine-2,4-dione moieties. EXPERT OPINION: The biological activity of compounds possessing a rhodanine moiety should be considered very critically despite the convincing data obtained in biological assays. In addition to the lack of selectivity, unusual structure-activity relationship profiles and safety and specificity problems mean that rhodanines are generally not optimizable.