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《合成通讯》2013,43(15):2635-2641
Abstract Convenient synthesis of uridine derivatives containing amino acid residues were carried out successfully by reacting triazolated uridine with the hydrochloride salts of some amino acid esters, which provides a general method for the direct introduction of amino acid group onto nucleoside residue. 相似文献
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Salama Tarek A. El-Ahl Abdel-Aziz S. Khalil Abdel-Galil M. Girges Margret M. Lackner Bernd Steindl Christian Elmorsy Saad S. 《Monatshefte für Chemie / Chemical Monthly》2003,134(9):1241-1252
Summary. Several new 1-aryl-, aralkyl-, and heteroaryl-5-(4-phenylbuta-1,3-dienyl)tetrazole derivatives and annulated tetrazole derivatives were efficiently and regiospecifically prepared in nearly quantitative yield via a facile one step reaction of dienones with a combination of tetrachlorosilane and sodium azide in acetonitrile under mild conditions. A complete structure assignment of three representative examples of the tetrazoles was achieved by advanced 2D NMR measurements including COSY, TOCSY, HSQC, HMBC, NOESY, and ROESY experiments.Received March 17, 2003; accepted March 18, 2003
Published online July 28, 2003 相似文献
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Tarek A. Salama Abdel-Aziz S. El-Ahl Abdel-Galil M. Khalil Margret M. Girges Bernd Lackner Christian Steindl Saad S. Elmorsy 《Monatshefte für Chemie / Chemical Monthly》2003,20(5):1241-1252
Several new 1-aryl-, aralkyl-, and heteroaryl-5-(4-phenylbuta-1,3-dienyl)tetrazole derivatives and annulated tetrazole derivatives were efficiently and regiospecifically prepared in nearly quantitative yield via a facile one step reaction of dienones with a combination of tetrachlorosilane and sodium azide in acetonitrile under mild conditions. A complete structure assignment of three representative examples of the tetrazoles was achieved by advanced 2D NMR measurements including COSY, TOCSY, HSQC, HMBC, NOESY, and ROESY experiments. 相似文献
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Vesna Kuntić Maja Stanojević Ivanka Holclajtner-Antunović Snežana Uskoković-Marković Ubavka Mioč Marija Todorović Tanja Jovanović Vladana Vukojević 《Monatshefte für Chemie / Chemical Monthly》2006,137(6):803-810
Summary. Compounds of phosphotungstic acid (WPA) containing the amino acids alanine (WPA–Ala) or glycine (WPA–Gly) as counter cations were synthesized and characterized by elemental analysis, thermal analysis, and IR spectroscopy. Cellular
toxicity was assessed by the trypan blue exclusion method, and the antiviral activity of WPA and the modified WPA compounds was tested against herpes simplex viruses (HSV) type 1 and type 2. Biological assays indicate that the newly synthesized
compounds exhibit no evident cytotoxic effects on Vero cells and negligible antiviral activity against HSV-1 and HSV-2. 相似文献
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Vesna Kunti? Maja Stanojevi? Ivanka Holclajtner-Antunovi? Sne?ana Uskokovi?-Markovi? Ubavka Mio? Marija Todorovi? Tanja Jovanovi? Vladana Vukojevi? 《Monatshefte für Chemie / Chemical Monthly》2006,43(9):803-810
Compounds of phosphotungstic acid (WPA) containing the amino acids alanine (WPA–Ala) or glycine (WPA–Gly) as counter cations were synthesized and characterized by elemental analysis, thermal analysis, and IR spectroscopy. Cellular
toxicity was assessed by the trypan blue exclusion method, and the antiviral activity of WPA and the modified WPA compounds was tested against herpes simplex viruses (HSV) type 1 and type 2. Biological assays indicate that the newly synthesized
compounds exhibit no evident cytotoxic effects on Vero cells and negligible antiviral activity against HSV-1 and HSV-2. 相似文献
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Muhammad Safadi Michael Chorev Eli Breuer 《Phosphorus, sulfur, and silicon and the related elements》2013,188(1-4)
Abstract Modified amino acids and peptides are in the focus of medicinal chemistry as potential mimics of natural compounds that may act as inhibitors and modulators of natural processes. Along with many other types of analogs, considerable effort was invested into the synthesis of phospha amino acids. Presently phospha analogs for all amino acids and for many peptides are known and some of these are of considerable practical importance. 相似文献
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含5-氟尿嘧啶的氨基酸衍生物的合成及其抗肿瘤活性研究 总被引:2,自引:0,他引:2
5-氟尿嘧啶乙酸对硝基苯酯和5-氟尿嘧啶丙酸对硝基苯酯与一系列氨基酸反应,制备了12个新的含5-氟尿嘧啶的氨基酸衍生物,并确定了化合物的结构。初步动物试验表明某些化合物有一定的抗肿瘤活性。 相似文献
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以保护L-谷氨酸(2)为原料,与N,N′-羰基二咪唑反应制得化合物3; 3与丙二酸单乙酯镁盐反应制得β-酮酯(4); 4分别与4-氟间苯二酚和4-氯间苯二酚进行Pechmann缩合后,在酸中脱除保护基合成了L-7-羟基香豆素氨基酸(1a)及其两个衍生物(1b, 35.3%和1c, 40.6%),其结构经1H NMR, 13C NMR和HR-MS(ESI)确证。采用UV-Vis研究了1b和1c的pKa。结果表明:1b和1c的pKa分别为6.21和6.14。两个衍生物的荧光性能与pH密切相关。 相似文献
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Ying Zhang Hui Yu Shuzheng Fu Luying Tan Junli Liu Baisong Zhou Le Li Yunhe Liu Caixia Wang Pingya Li Jinping Liu 《Molecules (Basel, Switzerland)》2021,26(4)
Aiming at seeking an effective anti-hepatocarcinoma drug with low toxicity, a total of 24 amino acid derivatives (20 new along with 4 known derivatives) of two active ocotillol-type sapogenins (pyxinol and ocotillol) were synthesized. Both in vitro and in vivo anti-hepatocarcinoma effects of derivatives were evaluated. At first, the HepG2 human cancer cell was employed to evaluate the anti-cancer activity. Most of the derivatives showed obvious enhanced activity compared with pyxinol or ocotillol. Among them, compound 2e displayed the most excellent activity with an IC50 value of 11.26 ± 0.43 µM. Next, H22 hepatoma-bearing mice were used to further evaluate the anti-liver cancer activity of compound 2e. It was revealed that the growth of H22 transplanted tumor was significantly inhibited when treated with compound 2e or compound 2e combined with cyclophosphamide (CTX) (p < 0.05, p < 0.01), and the inhibition rates of tumor growth were 35.32% and 55.30%, respectively. More importantly, compound 2e caused limited damage to liver and kidney in contrast with CTX causing significant toxicity. Finally, the latent mechanism of compound 2e was explored by serum and liver metabolomics based on ultra-performance liquid chromatography quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS) technology. A total of 21 potential metabolites involved in 8 pathways were identified. These results suggest that compound 2e is a promising agent for anti-hepato-carcinoma, and that it also could be used in combination with CTX to increase efficiency and to reduce toxicity. 相似文献
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Ebselen氨基酸衍生物的合成及抗脂质过氧化作用 总被引:19,自引:0,他引:19
Ebselen氨基酸衍生物的合成及抗脂质过氧化作用肖颖歆,刘秀芳,徐汉生,孙士勇,徐波(武汉大学化学系,武汉,430072)(北京医科大学天然药物及仿生药物国家重点实验室)关键词2-苯基-1,2-苯并异硒唑-3(2H)-酮,苯并异硒唑酮,氨基酸衍生物... 相似文献
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4-Ethoxyflavylium tetrafluoroborates with substituents in rings A and B were synthesized. Their reaction with nitrogen-containing nucleophiles was investigated. It was shown that derivatives of flavones at the carbonyl group are formed as a result of these reactions. The major distinctive physicochemical characteristics of the oximes of flavones and isoxazoles were determined. 相似文献
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Atom efficient, multicomponent reactions that lead to high-value products from inexpensive starting materials are of both economic and ecological interest for industrial organic synthesis. alpha-Amino acids are amongst the most important compounds in chemistry and biology. As well as their biochemical significance as building blocks of peptides and proteins, alpha-amino acids are also becoming increasingly interesting as fine chemicals. Possibly one of the key reactions in the preparation of these compounds is transition metal catalyzed amidocarbonylation, where the alpha-amino acid framework is constructed in a single step from an aldehyde, an amide, and carbon monoxide. This article gives a current overview of transition metal catalyzed amidocarbonylation reactions used in the synthesis of alpha-amino acids derivatives. A classification and summary of the significant features of this three component reaction is first presented together, with an historical introduction. This section is followed by two sections on cobalt- and palladium-catalyzed amidocarbonylation. A discussion of the mechanism of each of the different amidocarbonylation variants form an introduction. Overviews on further synthetic development of the methodology, such as the domino reaction with an amidocarbonylation step and the expansion of the range of starting materials, form the main topics of both variants. The potential of the method is demonstrated with the help of examples of special synthetic utility (for example, the preparation of arylglycines). Finally, possibilities for future developments in transition metal catalyzed amidocarbonylation reactions are proposed on the basis of the current state of knowledge. 相似文献
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Matthias Beller Markus Eckert Wahed A. Moradi Helfried Neumann 《Angewandte Chemie (International ed. in English)》1999,38(10):1454-1457
One-step synthesis of substituted hydantoins can be achieved by the palladium-catalyzed “ureidocarbonylation” of aldehydes with urea derivatives and carbon monoxide [Eq. (1)]. This surprisingly selective protocol converts substituted ureas into 1,5- and 1,3,5-substituted hydantoins in yields of up to 93 %. 相似文献
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The synthesis of three-dimensional cyclopentane amino acid derivatives with multiple stereocenters and with high regiochemical and diastereochemical diversity has been achieved starting from cyclopentadiene-derived β-aminocyclopentenecarboxylic acid. The small-molecular design was based on stereo- and regiocontrolled functionalization of the starting cyclopentene β-amino acid through stereoselective oxirane formation/regioselective oxirane opening and resulted in regio- and diastereoisomers of novel orthogonally protected aminocyclopentanecarboxylates. 相似文献
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