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天然产物结构复杂,生理活性独特,常被用作先导化合物,经过结构修饰和改造,发展为具有重要药用价值的化合物,在保障人类健康方面发挥重要的作用.近年来,具有独特立体结构、多修饰位点、良好生物相容性和生物活性的天然产物作为构筑单元,已应用到基于分子自组装的有机功能材料研究领域中.介绍以天然甾体、三萜、肽、糖等为结构骨架,设计合成的功能分子在有机凝胶方面的研究现状及其潜在的应用. 相似文献
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甾体化合物是一类生物体中广泛存在并起重要功能的生物分子。其特殊结构使这类化合物具有亲脂性,膜亲合性以及与低密度脂蛋白的特异性结合等性能。利用这些特性设计合成各种药物分子的甾体缀合物,可增加药物分子的脂溶性,提高跨膜渗透能力,在特定组织中的分布以及甾体缀合物自身具有独特的生物活性,对探索新型生物活性分子具有重要意义。本文介绍了近年来在设计合成新型甾体缀合物领域的研究进展,包括甾体药物缀合物、含磷甾体缀合物、作为离子通道和分子载体的缀合物及甾体二聚缀合物等。 相似文献
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《化学进展》2016,(Z2)
基于有机小分子多级自组装形成的超分子凝胶,由于其潜在的应用前景越来越受到人们的关注。合理设计凝胶因子并实现在适当的溶剂中自组装形成纤维状结构,对于分子识别和自组装来说都有一定挑战。三萜化合物具有独特的手性骨架结构,是一类重要的生物活性天然产物,在消炎、降血脂、保肝护肾、抗菌、抗肿瘤、抗真菌等方面有着重要的药用价值。近年来,基于独特的手性刚性骨架和具有多个可修饰位点的特点,此类化合物的聚集性质和在超分子组装方面的应用已经引起关注。本文总结了未经修饰的五环三萜化合物的聚集组装性质和基于此类骨架的功能分子在超分子凝胶方面的研究,并介绍了此类超分子凝胶潜在的应用。结果表明,发展基于此类天然产物骨架的超分子组装体,不仅为超分子凝胶的研究引入新的构筑基元,并且能够达到阐述生物活性分子之间相互作用力以及充分利用自然界资源创造新材料的目的。 相似文献
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环糊精是超分子化学中的一类重要主体化合物,在药物缓释、化学传感、对映体分离以及新型材料等众多领域都得到了广泛的应用.由于环糊精具有外亲水内疏水的桶形结构,其空腔内可以插入具有识别功能的受体分子或荧光染料,可通过螯合或置换方式实现对目标分子的识别,因此基于环糊精衍生物及包合物构建荧光探针也受到了人们的极大关注.总结了基于环糊精设计合成的荧光探针在检测金属离子、阴离子和分子等方面的应用,重点描述了识别性能和识别机制,为环糊精衍生物及包合物在荧光检测领域的应用提供理论依据. 相似文献
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咔唑类化合物研究新进展 总被引:17,自引:0,他引:17
咔唑及其衍生物是一类重要的含氮芳杂环化合物,分子内含有较大的共轭体系和强的分子内电子转移,这种特殊的刚性稠环结构使咔唑类化合物表现出许多独特的性能及生物活性,在光电材料、染料、医药、超分子识别等多领域具有潜在的广泛应用.更为重要的是咔唑类化合物易于进行结构修饰,在咔唑环上可方便地引入各种功能基,咔唑衍生物的合成及其开拓咔唑类化合物潜在的新用途,成为近些年来十分活跃的研究领域,且发展迅速.结合自己的工作,参考国内外文献,全面综述了咔唑类化合物在有机电致发光材料、光折变材料、太阳能电池材料、染料、医药和超分子识别等领域的研究与开发新进展,并对其发展趋势作了展望. 相似文献
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氢键识别超分子聚合物的新进展* 总被引:1,自引:0,他引:1
近年来,由于氢键作用对聚合物的热力学性质、微观自组装、结晶及液晶行为的重要影响,氢键识别在超分子聚合物的分子设计与结构控制方面的应用受到广泛关注。本文系统介绍了氢键识别体系的类型与性质,以及分子结构、分子内氢键对氢键识别强度的影响,讨论了羧酸与吡啶间氢键识别体系、与核苷相关的氢键识别体系以及四重氢键识别体系在超分子聚合物中的最新应用,主要介绍了氢键识别超分子聚合物的合成、结构、性质及功能。 相似文献
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用FTIR研究环氧化天然橡胶的热老化 总被引:1,自引:0,他引:1
从合成结构新颖的杂环化合物角度出发,寻找具有较好生物活性的新物质,是研究新农药的一个重要方向[1].最近研究表明很有可能从异噻唑杂环中找到生物活性独特的新型化合物[2].据报道,腙类化合物具有很好的生物活性[3].我们设计合成了含异噻唑杂环的腙类新型... 相似文献
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Two new triterpenoid saponins, named ginsenoside Rh10 (1) and notoginsenoside ST-6 (2), were isolated from notoginseng medicinal fungal substance. Their structures were elucidated by a combination of 1D and 2D NMR, MS and chemical analysis. 相似文献
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Cussonia holstii is a traditional medicinal plant used in Kenya, which has not been studied chemically up-to-date. Upon biological screening, a substantial antitrichomonas activity was found in the dichloromethane extract of the bark of Cussonia holstii. A detailed chromatographic study using centrifugal partition chromatography revealed that a pentacyclic triterpenoid, i.e., hederagenin, is the antitrichomonas constituent of the plant with a IC50 of 2.8 microM. 相似文献
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Xiu-xiu Dou Shan Lin Xin-hui Tian Yu-hao Zhang Xin Guo Ji Ye Wei-dong Zhang 《Biomedical chromatography : BMC》2020,34(10):e4914
Dingkun Dan (DKD), a famous traditional Chinese medicine, has been widely used in the treatment of irregular menstruation, leucorrhea abnormality, and postpartum gynecological diseases since Qing dynasty (1739). It comprises 30 flavors of Chinese medicinal materials, which results in its complex chemical composition. In this study, an integrative method was developed to rapidly characterize the chemical components of DKD using ultra-high-performance liquid chromatography quadrupole time-of-flight mass spectrometry combined with the UNIFI™ software. A total of 234 compounds, including 47 triterpenoid saponins, 55 flavonoids, and 38 alkaloids, were identified. Of them, 170 compounds were characterized initially and 61 compounds were identified unambiguously using reference standards. Under the same analysis conditions, 43 prototypical components, which were tentatively assigned as triterpenoid saponins, flavonoids, alkaloids, terpenoids, phenylpropanoids, and others, were absorbed in rat by serum pharmacochemistry analysis. DKD exhibited diverse pharmacological activities through the combined effect of these components. This study was the first systematic study of chemical components in vitro originating from 30 medicinal materials and prototypes in vivo of DKD, which could provide scientific evidence for explaining its therapeutic effect. 相似文献
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One new triterpenoid saponin,monepaloside K(1) was isolated from the water-soluble part of the whole plant of a famous Tibetan medicinal herb,morina neplaensis var. alba Hand.-Mazz.Its structure was determined to be 3-O-α-L-arabinopyranosyl-(1→3)-β-D-xylopyranosyl siaresinolic acid on the basis of spectroscopic evidences,especially 2D NMR techniques. 相似文献
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Dr. Ulrich Lücking 《Chemistry (Weinheim an der Bergstrasse, Germany)》2022,28(56):e202201993
Extension of the medicinal chemistry toolbox is in the vital interest of drug designers. However, the diffusion of an innovation can be a lengthy process. Along these lines, it took almost 70 years before the use of the sulfoximine group reached a critical mass in medicinal chemistry. Even though interest in this versatile functional group has increased exponentially in recent years, there is ample room for further innovative applications. This Review highlights emerging trends and opportunities for drug designers for the utilization of the sulfoximine group in medicinal chemistry, such as in the construction of complex molecules, proteolysis targeting chimeras (PROTACs), antibody-drug conjugates (ADCs) and novel warheads for covalent inhibition. 相似文献
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Tetrazoles and acyl sulfonamides are functional groups that are common in medicinal chemistry but virtually unexplored as recognition elements in supramolecular chemistry. We report here on the anion binding properties of these highly acidic N-H functional groups. We have prepared two new calixarene-based tetrazole-containing hosts, as well as new acetyl sulfonamide and benzoyl sulfonamide hosts. We also report on analogous hosts bearing the better-known aryl sulfonamide functional group as a point of comparison. We find that these hosts are competent anion binders and that the recognition of anions by these groups is highly dependent on their conformational preferences. We also report in detail on the preferred molecular shape of each acid bioisostere as determined by calculations and structural database surveys, and discuss how these shapes impact binding in the context of the reported hosts. 相似文献
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Vuyolwethu Khwaza Sithenkosi Mlala Opeoluwa O. Oyedeji Blessing A. Aderibigbe 《Molecules (Basel, Switzerland)》2021,26(9)
Pentacyclic triterpenoids are well-known phytochemicals with various biological activities commonly found in plants as secondary metabolites. The wide range of biological activities exhibited by triterpenoids has made them the most valuable sources of pharmacological agents. A number of novel triterpenoid derivatives with many skeletal modifications have been developed. The most important modifications are the formation of analogues or derivatives with nitrogen-containing heterocyclic scaffolds. The derivatives with nitrogen-containing heterocyclic compounds are among the most promising candidate for the development of novel therapeutic drugs. About 75% of FDA-approved drugs are nitrogen-containing heterocyclic moieties. The unique properties of heterocyclic compounds have encouraged many researchers to develop new triterpenoid analogous with pharmacological activities. In this review, we discuss recent advances of nitrogen-containing heterocyclic triterpenoids as potential therapeutic agents. This comprehensive review will assist medicinal chemists to understand new strategies that can result in the development of compounds with potential therapeutic efficacy. 相似文献
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S-Monofluoromethyl phosphorothioates represent an important class of organofluorine compounds and are re ported here for the first time.A series of S-monofluoromethyl phosphorothioates are conveniently synthesized from different PⅤ-H compounds and PhSO2SCH2F under mild conditions.The method is compatible with common functional groups and provides potential opportunities to synthesize new bioactive molecules for medicinal chemistry. 相似文献