Synthesis and antibacterial activity of novel 11,12-cyclic carbonate azithromycin 4''-O-carbamate derivatives.

Ma C; Liu Z; Song H; Jiang R; He F; Ma S

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Synthesis and antibacterial activity of novel 11,12-cyclic carbonate azithromycin 4''-O-carbamate derivatives.

机译：新型11,12环碳酸二十霉素4'' - 氨基甲酸酯衍生物的合成及抗菌活性。

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A series of novel 11,12-cyclic carbonate azithromycin 4''-O-carbamate derivatives were designed, synthesized and evaluated for their in vitro antibacterial activities. Compounds 7b and 7d were the most effective (0.5 and 0.5 microg ml(-1)) against two strains of erythromycin-resistant Streptococcus pneumoniae whose resistance was encoded by the erm gene and the erm and mef genes, respectively. Compounds 7a, 7e and 7g showed significantly potent activity against erythromycin-susceptible strains such as Staphylococcus aureus and S. pyogenes. These results suggest that the introduction of the prolonged arylalkylcarbamoyl group to the C-4'' position can dramatically enhance the activity against erythromycin-resistant bacteria encoded by the erm gene or the erm and mef genes.

机译：设计，合成和评估了一系列新的11,12环碳酸二十霉素4' - 氨基甲酸酯衍生物，用于其体外抗菌活性。化合物7B和7D是最有效的（0.5和0.5微毫升ML（-1）），其两种红霉素抗性链球菌肺炎群菌株分别由ERM基因和ERM和MEF基因分别编码。化合物7A，7E和7G针对红霉素易感菌株如葡萄球菌和S. PEOGONES的菌株显示出显着的活性活性。这些结果表明，将延长的芳基烷基羰基酰基与C-4'位置的引入可以显着增强对由ERM基因或ERM和MEF基因编码的抗红霉素抗性细菌的活性。

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《The Journal of Antibiotics: An International Journal》 |2010年第1期|共6页
作者
Ma C; Liu Z; Song H; Jiang R; He F; Ma S;
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Department of Medicinal Chemistry School of Pharmaceutical Sciences Shandong University Jinan PR China.;

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正文语种 eng
中图分类药学;
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1. Synthesis and antibacterial activity of novel 11,12-cyclic carbonate azithromycin 4''-O-carbamate derivatives. [J] . Ma C, Liu Z, Song H, The Journal of Antibiotics: An International Journal . 2010,第1期

机译：新型11,12-环碳酸阿奇霉素4''-O-氨基甲酸酯衍生物的合成和抑菌活性。
2. Synthesis and antibacterial activity of novel 11,12-cyclic carbonate azithromycin 4''-O-carbamate derivatives. [J] . Ma C, Liu Z, Song H, The Journal of Antibiotics: An International Journal . 2010,第1期

机译：新型11,12环碳酸二十霉素4'' - 氨基甲酸酯衍生物的合成及抗菌活性。
3. Synthesis and antibacterial activity of new 4''-O-carbamates of 11,12-cyclic carbonate erythromycin A 6,9-imino ether. [J] . Zhang L, Jiao B, Yang X, The Journal of Antibiotics: An International Journal . 2011,第3期

机译：11,12-环状碳酸红霉素A 6,9-亚氨基醚的新型4''-O-氨基甲酸酯的合成和抗菌活性。
4. Himic anhydride and its derivatives. Synthesis oxygen- and nitrogen containing cyclic systems [C] . V.A. Palchikov, I.N. Tarabara, L.I. Kasyan European Symposium on Organic Chemistry . 2009

机译：Hemic酸酐及其衍生物。合成含氧氧循环系统
5. Synthesis of side chain-modified iodothyronines. Synthesis and structure-activity relationships (SARS) of galanthamine derivatives. Total synthesis of (+)-valyldetoxinine. Synthesis and mechanism of cyclic acetal and ketal formation in pentono-1,4-lactones. [D] . Han, So-Yeop. 1992

机译：侧链修饰的碘甲状腺素的合成。加兰他敏衍生物的合成及其构效关系（SARS）。（+）-Valyldetoxinine的全合成。戊通-1,4-内酯中环状缩醛和缩酮的合成及其机理。
6. Synthesis and Antibacterial Evaluation of a Series of 1112-Cyclic Carbonate Azithromycin-3-O-descladinosyl-3-O-carbamoyl Glycosyl Derivatives [O] . Chao-Ming Wang, Feng-Lan Zhao, Lei Zhang, 2017

机译：一系列1112-环碳酸酯类阿奇霉素-3-O-癸二糖基-3-O-氨基甲酰基糖基糖基衍生物的合成及抗菌评价
7. Synthesis and Antibacterial Evaluation of a Series of 11,12-Cyclic Carbonate Azithromycin-3-O-descladinosyl-3-O-carbamoyl Glycosyl Derivatives [O] . Chao-Ming Wang, Feng-Lan Zhao, Lei Zhang, 2017

机译：一系列11,12-环碳酸酯阿奇霉素-3-O-去甲肾上腺素-3-O-氨基甲酰基糖基衍生物的合成和抗菌评价

Synthesis and antibacterial activity of novel 11,12-cyclic carbonate azithromycin 4''-O-carbamate derivatives.

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