排序方式: 共有37条查询结果,搜索用时 31 毫秒
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Dr. Kevin Neumann Alessia Gambardella Prof. Mark Bradley 《Chembiochem : a European journal of chemical biology》2019,20(7):872-876
Traditionally, prodrug activation has been limited to enzymatic triggers or gross physiological aberrations, such as pH, that offer low selectivity and control over dosage. In recent years, the field of prodrug activation chemistry has been transformed by the use of bioorthogonal reactions that can be carried out under biological conditions at sub-millimolar concentrations, with the tetrazine-mediated inverse electron demand Diels–Alder reaction amongst the most recognised. Their high reaction rates, chemoselectivity and excellent biocompatibility make tetrazines ideal small molecules for activating prodrugs. Recently the tetrazine moiety has been used as a prodrug for a pyridazine thus broadening the scope of prodrug systems. This article discusses the concept of using tetrazines as small-molecule activators for prodrugs, and provides an overview of tetrazine-based prodrug systems, with a particular focus on the recently reported prodrug–prodrug activation strategy. 相似文献
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四嗪类高氮分子及离子含能化合物的研究进展 总被引:2,自引:0,他引:2
详细论述了近年来国内外报道的四嗪类高氮分子及离子含能化合物的合成与性能研究,指出部分化合物由于其生成焓高、热稳定性好以及感度低等特点在含能材料领域具有广泛的应用前景.同时还总结了目前四嗪类含能化合物普遍存在的问题及以后的发展方向. 相似文献
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Coordination‐Assisted Bioorthogonal Chemistry: Orthogonal Tetrazine Ligation with Vinylboronic Acid and a Strained Alkene 下载免费PDF全文
Selma Eising Dr. Bo‐Tao Xin Fleur Kleinpenning Jurriaan J. A. Heming Dr. Bogdan I. Florea Prof. Dr. Herman S. Overkleeft Dr. Kimberly M. Bonger 《Chembiochem : a European journal of chemical biology》2018,19(15):1648-1652
Bioorthogonal chemistry can be used for the selective modification of biomolecules without interfering with any other functionality that might be present. Recent developments in the field include orthogonal bioorthogonal reactions to modify multiple biomolecules simultaneously. During our research, we observed that the reaction rates for the bioorthogonal inverse‐electron‐demand Diels–Alder (iEDDA) reactions between nonstrained vinylboronic acids (VBAs) and dipyridyl‐s‐tetrazines were exceptionally higher than those between VBAs and tetrazines bearing a methyl or phenyl substituent. As VBAs are mild Lewis acids, we hypothesised that coordination of the pyridyl nitrogen atom to the boronic acid promoted tetrazine ligation. Herein, we explore the molecular basis and scope of VBA–tetrazine ligation in more detail and benefit from its unique reactivity in the simultaneous orthogonal tetrazine labelling of two proteins modified with VBA and norbornene, a widely used strained alkene. We further show that the two orthogonal iEDDA reactions can be performed in living cells by labelling the proteasome by using a nonselective probe equipped with a VBA and a subunit‐selective VBA bearing a norbornene moiety. 相似文献
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国外四嗪四唑类高氮含能材料研究进展 总被引:28,自引:12,他引:16
对国外正在研究的四嗪、四唑类高氮含能材料进行了综述,介绍了部分四嗪、四唑类高氮化合物及其衍生物的合成、理化性质和应用前景,对国外研究的3,6-二肼基-1,2,4,5-四嗪(DHT)、3,3′-偶氮(6-氨基-1,2,4,5-四嗪)(DAAT)、3,6-双(1氢-1,2,3,4-四唑-5-氨基)-1,2,4,5-四嗪(BTATz)、联四唑(BHT)等进行了重点描述。 相似文献
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We report the synthesis of polyurethane‐urea elastomers containing 1,2,4,5‐tetrazine covalently reacted within the main chains of the polymers. Our study investigates the synthesis of 3,6‐diamino‐1,2,4,5‐tetrazine (DAT), the polymerization reaction conditions for reacting DAT into the backbone of segmented polyurethane elastomers, and the metal‐complexation capabilities of tetrazine‐containing elastomers with cobalt (II) chloride. Tetrazines are highly colored and electro‐active heterocyclic moieties, which have a very high electron affinity which make them reducible at high to very high potentials. Upon complexation with metals, we observed a strong color shift of the polymers from deep red to blue indicating the binding efficacy for the polymers. We quantified the metal‐complexation capability of the tetrazine elastomers and determined a molar ratio of approximately two metal atoms per tetrazine allowing us to provide a plausible complexation mechanism for the active polymers. © 2009 Wiley Periodicals, Inc. J Appl Polym Sci, 2009 相似文献
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《Journal of Sulfur Chemistry》2013,34(6):605-615
Derivatives containing the cyclohepta4′,5′thieno[2′,3′:4,5]pyrimido[1,2-b][1,2,4,5]-tetrazin-6-one system were prepared from the reaction of 3-amino-2-thioxo-1,2,3,5,6,7,8,9-octahydro-4H-cyclohepta[4,5]thieno[2,3-d]pyrimidin-4-one (5) or its 2-methylthio derivative 6 with hydrazonoyl chlorides 9. The mechanism of the studied reactions has been discussed and the biological activity of the isolated products has been evaluated. 相似文献
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以3?氨基?4(?叔丁基?NNO?氧化偶氮基)呋咱(ABAo F)为原料,经重氮化开环、肟化、氧化、氨化和硝化环化五步反应得到目标化合物1?羟基?1,2,3?三唑并[4,5?e]?5,7?二氧化?1,2,3,4?四嗪(HTTDO),总收率24.1%,采用红外光谱、核磁共振、质谱及元素分析对中间体及产物的结构进行了表征;探讨了氨化及硝化环化的反应机理;培养了HTTDO·4.5H2O的单晶,X射线衍射分析表明,其为正斜方晶系,空间群为Pna2(1),晶体密度为1.659 g·cm~(-3);利用Gaussian 09程序和Kamlet?Jacobs方程计算HTTDO理论密度为1.88 g·cm~(-3),爆速为9393 m·s-1,爆压为41.9 GPa,爆热为8010 J·g~(-1);采用差示扫描量热(DSC)研究了HTTDO的热性能:其在热分解过程中,放热剧烈,峰温最高达194.5℃。 相似文献
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Karl O. Christe David A. Dixon Monica Vasiliu Ross I. Wagner Ralf Haiges Jerry A. Boatz the late Herman L. Ammon 《Propellants, Explosives, Pyrotechnics》2015,40(4):463-468
Theoretical calculations were carried out for the isomeric di‐1,2,3,4‐tetrazine tetraoxides (DTTO and iso‐DTTO). The most important explosion performance parameters, the detonation pressure and detonation velocity, are dominated by the densities and not by the heats of formation of these compounds. Since DTTO and iso‐DTTO are unknown, reliable predictions of their crystal densities are crucial for an evaluation of the potential of these materials as explosives. In this study, the crystal densities were predicted using both Ammon’s Atom/Functional Group and Atom Code Volume Additivity Parameters and Quantum Mechanical molecular Volume methods, resulting in similar densities and explosion parameters. Although the likely uncertainties in our predicted density values are difficult to assess due to a lack of experimental data for closely related known compounds, our results demonstrate that Shechter’s originally proposed densities and performance parameters were grossly overestimated. Furthermore, it is shown that, based on our predicted density value ranges, DTTO and iso‐DTTO could match or substantially outperform the best state of the art explosives, such as CL‐20. Therefore, the synthesis of DTTO and iso‐DTTO should be further pursued. 相似文献
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