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G. J. Koomen J. B.M. Van Rhijn U. K. Pandit 《Nucleosides, nucleotides & nucleic acids》2013,32(1-2):215-216
Abstract The synthesis and the chemical and biological properties of several non-glycosidic derivatives of 5-fluorouracil are described. 相似文献
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合成了一系列3-羟基-4(1H)-吡啶酮类衍生物,并研究了它们对5-脂氧合酶的抑制作用. 发现6-取代-3-羟基-4(1H)-吡啶酮化合物(2a~2e)对5-脂氧合酶具有显著抑制作用, 特别是6-苯硫基-1-苯基-2-甲基-3-羟基-4(1H)-吡啶酮(2a)的抑制效果最好(IC50=2.52 μmol/L). 6-位没有取代基的羟基吡啶酮类化合物对5-脂氧合酶却没有抑制作用. 讨论了6-取代-3-羟基-4(1H)-吡啶酮类化合物对5-脂氧合酶的抑制作用机制. 相似文献
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The antibacterial activity of several new 5-aminoorotic acid derivatives considered as possible competitors of orotate towards
dihydroorotase has been investigated. Products with a bromacetamido substitution demonstrated antibacterial properties. However,
the paradoxical behavior of some compounds in synthetic media, opposed to the expected results obtained with an E. coli strain lacking dehydroorotic dehydrogenase, did not allow us to draw conclusions on their mechanism of action. 相似文献
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Kiyoshi Isono Saburo Suzuki Michio Tanaka Takeo Nanbata Kunitoyo Shibuya 《Bioscience, biotechnology, and biochemistry》2013,77(9):1571-1579
5-Carboxyuracil derivatives were shown to react with aqueous sodium bisulfite in mild condition resulting in facile decarboxylation to give corresponding 5-decarboxy-5,6-dihydrouracil-6-sulfonates and uracils in good yield. The former compounds were quantitatively transformed to the latter in alkaline condition. Mechanistic feature of this reaction was discussed, which implied the initial nucleophilic addition of bisulfite across the 5,6-double bond. 5-Carboxycytosine was also shown to react similarly, however, accompanied by hydrolytic deamination. 相似文献
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S. Ozaki Y. Watanabe T. Nagase T. Ogasawara S. Ahmad A. Hoshi 《Nucleosides, nucleotides & nucleic acids》2013,32(1-2):249-256
Abstract 1-Carbonyl 5-fluorouracil derivatives,5′-acyl-5-fluorouridines, and 5-fluorouridilic acid esters were synthesized and their antitumor activities were tested. 相似文献
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Andronova V. L. Skorobogatyi M. V. Manasova E. V. Berlin Yu. A. Korshun V. A. Galegov G. A. 《Russian Journal of Bioorganic Chemistry》2003,29(3):262-266
5-(3-Perylenylethynyl)-2'-deoxyuridine was prepared by crosslinking 5-iodo-2'-deoxyuridine derivatives with 3-ethynylperylene followed by deprotection. 5-(1-Perylenylethynyl)-, 5-(3-perylenylethynyl)-, and 5-[4-(2-benzoxazolyl)phenylethynyl]-2'-deoxyuridine were found to inhibit in Vero cells the replication of type 1 herpes simplex virus and its drug-resistant strains. 相似文献
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Lawrence C. Davies 《Nucleosides, nucleotides & nucleic acids》2013,32(3):395-400
Abstract Two novel nucleoside derivatives,5′-0-aminothymidine and 5′-deoxy-5′-hydrazinothymidine were synthesised as potential thymidine kinase inhibitors. The former was made from N-hydroxyu re thane and 5′-0-tosylthymidine and the latter from benzyl carbazate and 5′-0-tosylthymidine. 相似文献
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5-Fluorouracil (FU), 5-fluorocytosine, and the riboside and deoxyriboside derivatives of these fluoropyrimidines each exhibit a different spectrum of inhibitory effects in pneumococci. The biochemical basis of this finding seems to be the extremely low level of nucleoside phosphorylase (hydrolase) and N-trans-deoxyribosylase activity in pneumococcus and the consequent, relatively limited metabolic interconversion of the different fluoropyrimidines, which can therefore selectively affect one or the other of the several drug-sensitive biochemical reactions in this bacterium. Special attention was paid to the effect of fluoropyrimidines on the metabolism of cytosine and thymidine. In spite of the fact that FU is converted to both fluorouridine triphosphate and fluorocytidine triphosphate, only fluorouridylate but no fluorocytidylate can be detected in the ribonucleic acid Exogenous FU and fluorouridine also inhibit the synthesis of cytosine nucleotides from supplied uridine in a pyrimidine auxotroph. Thymidine was found to be a poor reversing agent for any of the fluoropyrimidine inhibitions. In both the wild type and in a thymidine-requiring (thymidylate-synthetase deficient) mutant, growing with supplied thymidine in the medium, fluorodeoxyuridine (FUdR) treatment caused cell death and inhibition of the incorporation of radioactive thymidine, adenosine, or uracil into deoxyribonucleic acid. It is suggested that FUdR (or a metabolic derivative) inhibits the transport of phosphorylation of thymidine in this microorganism. 相似文献
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V. A. Korshun E. V. Manasova K. V. Balakin A. D. Malakhov A. V. Perepelov T. A. Sokolova 《Nucleosides, nucleotides & nucleic acids》2013,32(9-11):1809-1812
Abstract Four fluorescent nucleosides, 5-(4-pyrenylethynyl)-, 5-(l-pyrenylbutadiynyl)-, 5-(3-perylenylethynyl)-, and 5-[4-(2-benzoxazolyl)phenylethynyl]-2′-deoxyuridines, were synthesized. 相似文献
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Propanal thiosemicarbazone (1a) showed activity in preventing anaphylactic shock in a mouse test-system; it also had some activity in stunting the growth of Botrytis allii. Hexanal thiosemicarbazone (1b) was active in the Botrytis allii test-system, and citral thiosemicarbazone (2) and citral guanylhydrazone nitrate (3) showed some activity in the same test-system. Heptanal guanylhydrazone nitrate (4) had some antibacterial activity against Staphylococcus aureus, and D-threo-pentosulose bis(thiosemicarbazone) (5) prevented anaphylactic shock in the mouse test-system. D-glycero-Tetrosulose bis(thiosemicarbazone) (6), D-lyxo-hexosulose bis-(guanylhydrazone) nitrate (7), D-galacto-heptosulose bis(thiosemicarbazone) (8), and D-galacto-heptosulose bis(guanylhydrazone) sulfate (9) showed some activity in stunting the growth of Botrytis allii. The copper chelate (10a) of D-arabino-hexosulose bis(thiosemicarbazone), and the copper (11a) and palladium (11b) chelates of 6-deoxy-L-arabino-hexosulose bis(thiosemicarbazone) showed antitumor activity in the KB cell-culture test-system. The palladium chelate 11b also showed some activity in the leukemia p-388 mouse test-system. 相似文献
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Noreen L. Lyell Anne K. Dunn Jeffrey L. Bose Susan L. Vescovi Eric V. Stabb 《Applied microbiology》2008,74(22):7059-7063
We have developed a transposon mutagenesis system for Vibrio fischeri ES114 that utilizes a hyperactive mutant Tn5 transposase (E54K and M56A) and optimized transposon ends. Using a conjugation-based procedure, we obtained independent single-insertion mini-Tn5 mutants at a rate of ~10−6. This simple and inexpensive technique represents a significant improvement over previous methods for transposon mutagenesis of V. fischeri and should be applicable to many other bacteria. 相似文献
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Negrya S. D. Makarov D. A. Solyev P. N. Karpenko I. L. Chekhov O. V. Glukhova A. A. Vasilyeva B. F. Sumarukova I. G. Efremenkova O. V. Kochetkov S. N. Alexandrova L. A. 《Russian Journal of Bioorganic Chemistry》2020,46(2):133-138
Russian Journal of Bioorganic Chemistry - To obtain nucleoside derivatives with antibacterial activity, we have proposed three ways of the synthesis of 5-alkylthiomethyl-2'-deoxyuridines, which... 相似文献
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Luciana M. Leo Suellen Almeida-Corrêa Claudio A. Canetti Olavo B. Amaral Fernando A. Bozza Fabricio A. Pamplona 《PloS one》2014,9(1)
When 5-lipoxygenase (5-LO) is inhibited, roughly half of the CNS effect of the prototypic endocannabinoid anandamide (AEA) is lost. Therefore, we decided to investigate whether inhibiting this enzyme would influence physiological functions classically described as being under control of the endocannabinoid system. Although 5-LO inhibition by MK-886 reduced lipoxin A4 levels in the brain, no effect was found in the elevated plus maze (EPM), even at the highest possible doses, via i.p. (10 mg/kg,) or i.c.v. (500 pmol/2 µl) routes. Accordingly, no alterations in anxiety-like behavior in the EPM test were observed in 5-LO KO mice. Interestingly, aged mice, which show reduced circulating lipoxin A4 levels, were sensitive to MK-886, displaying an anxiogenic-like state in response to treatment. Moreover, exogenous lipoxin A4 induced an anxiolytic-like profile in the EPM test. Our findings are in line with other reports showing no difference between FLAP KO or 5-LO KO and their control strains in adult mice, but increased anxiety-like behavior in aged mice. We also show for the first time that lipoxin A4 affects mouse behavior. In conclusion, we propose an age-dependent relevancy of endogenous 5-LO derivatives in the modulation of anxiety-like behavior, in addition to a potential for exogenous lipoxin A4 in producing an anxiolytic-like state. 相似文献
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Chao Gao Dai Honglin Si Xiaojie Zhang Yutong Liu Limin Wang Zhengjie Meng Yaqi Zhang Yang Wang Tao Zheng Jiaxin Shan Lihong Liu Hongmin Zhang Qiurong 《Russian Journal of Bioorganic Chemistry》2022,48(2):411-422
Russian Journal of Bioorganic Chemistry - In order to discover novel high efficiency and low toxic anticancer drugs, a series of novel 2-amino-5-ethylpyrimidine derivatives (XIIa–x) were... 相似文献
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胡椒碱及其衍生物对SH-SY5Y细胞的保护作用研究 总被引:1,自引:0,他引:1
对胡椒碱进行结构改造,合成了4个胡椒碱衍生物。以高浓度皮质酮(corticosterone)模拟抑郁及焦虑症神经细胞损伤状态。对包括胡椒碱在内的5个化合物进行了SH-SY5Y细胞保护作用的研究。结果表明:胡椒碱、5-(3,4-methylenedioxy phenyl)-2E,4E-pentadienoic acid n-propylamine amide(2)以及5-(3,4-methylenedioxyphenyl)-2E,4E-pentadienoic acid N-methyl piperazine amide(4)对SH-SY5Y细胞有较好的保护作用。其中化合物2对SH-SY5Y细胞具有明显和持久的保护作用。 相似文献
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《Nucleosides, nucleotides & nucleic acids》2013,32(5-8):981-985
Abstract 5′-Aminocarbonylphosphonyl and aminocarbonylmethylphosphonyl diesters of AZT and d4T were synthesized as potential anti-HIV agents. 相似文献
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5- 氟尿嘧啶靶向衍生物的研究进展 总被引:1,自引:0,他引:1
李楠陈曦梁蓉梅江婉雍小兰 《现代生物医学进展》2011,11(13):2581-2583
5-氟尿嘧啶是目前临床上的一线抗肿瘤药物之一,其抗瘤谱广,为高效抗代谢药物,但其首过代谢明显,毒副作用大,治疗剂量与中毒剂量接近,且口服吸收不稳定,半衰期短。因此,对5-氟尿嘧啶进行有效的分子修饰,以克服其缺点,提高其靶向性,最大程度地发挥其活性作用和减轻毒副作用,已成为当今抗癌药物研究的热点。本文根据不同靶向载体,对近年来国内外各种分子修饰的5-氟尿嘧啶靶向衍生物及其抗肿瘤活性研究进行综述。 相似文献