Synthesis and antibacterial activity of novel 15-membered macrolide derivatives: 4''-carbamate, 11,12-cyclic carbonate-4''-carbamate and 11,4''-di-O-arylcarbamoyl analogs of azithromycin.

Ma S; Ma R; Liu Z

首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and antibacterial activity of novel 15-membered macrolide derivatives: 4''-carbamate, 11,12-cyclic carbonate-4''-carbamate and 11,4''-di-O-arylcarbamoyl analogs of azithromycin.

【24h】

Synthesis and antibacterial activity of novel 15-membered macrolide derivatives: 4''-carbamate, 11,12-cyclic carbonate-4''-carbamate and 11,4''-di-O-arylcarbamoyl analogs of azithromycin.

机译：新型15元大环内酯衍生物的合成和抗菌活性：阿奇霉素的4''-氨基甲酸酯，11,12-环状碳酸酯-4''-氨基甲酸酯和11,4''-二-O-芳基氨基甲酰基类似物。

获取原文

获取原文并翻译 | 示例

掌桥外文数据库（机构版） >>

开具论文收录证明 >>

文献代查 >>

页面导航

摘要
著录项
相似文献
相关主题

摘要

4''-Carbamate, 11,12-cyclic carbonate-4''-carbamate and 11,4''-di-O-arylcarbamoyl analogs of azithromycin were designed, synthesized and evaluated. The 4''-carbamate analogs retained excellent activity against erythromycin-susceptible Staphylococcus pneumoniae and showed improved activity against erythromycin-resistant Staphylococcus pneumoniae. Compared with 4''-carbamate analogs, 11,12-cyclic carbonate-4''-carbamate analogs exhibited improved activity against erythromycin-resistant Staphylococcus pneumoniae encoded by the mef gene or the erm and mef genes, and 11,4''-di-O-arylalkylcarbamoyl analogs showed greatly improved activity (0.25-0.5 microg/mL) against erythromycin-resistant Staphylococcus pneumoniae encoded by the erm gene. Among them, the novel series of 11,4''-di-O-arylalkylcarbamoyl analogs 7a-k exhibited potent and balanced activity against susceptible and resistant bacteria. In particular, compounds 7f and 7k were the most effective against susceptible bacteria and resistant bacteria encoded by the erm gene or the mef gene.

机译：设计，合成和评估了阿奇霉素的4''-氨基甲酸酯，11,12-环状碳酸酯-4''-氨基甲酸酯和11,4''-二-O-芳基氨基甲酰基类似物。 4''-氨基甲酸酯类似物保留了对易患红霉素的肺炎金黄色葡萄球菌的优异活性，并显示了对抵抗红霉素的肺炎性葡萄球菌的改良活性。与4''-氨基甲酸酯类似物相比，11,12-环状碳酸酯-4''-氨基甲酸酯类似物对由mef基因或erm和mef基因编码的抗红霉素的肺炎葡萄球菌和11,4''-表现出更高的活性。二-O-芳基烷基氨基甲酰基类似物对由erm基因编码的抗红霉素的肺炎葡萄球菌具有显着改善的活性（0.25-0.5 microg / mL）。其中，新颖的11,4''-二-O-芳基烷基氨基甲酰基类似物系列7a-k对敏感和耐药细菌表现出有效且平衡的活性。特别地，化合物7f和7k对由erm基因或mef基因编码的易感细菌和抗性细菌最有效。

著录项

来源
《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2009年第10期|共11页
作者
Ma S; Ma R; Liu Z;
展开▼
作者单位

展开▼
收录信息
原文格式 PDF
正文语种 eng
中图分类医药、卫生;劳动卫生;
关键词

相似文献

外文文献
中文文献
专利

1. Synthesis and antibacterial activity of novel 15-membered macrolide derivatives: 4''-carbamate, 11,12-cyclic carbonate-4''-carbamate and 11,4''-di-O-arylcarbamoyl analogs of azithromycin. [J] . Ma S, Ma R, Liu Z European Journal of Medicinal Chemistry: Chimie Therapeutique . 2009,第10期

机译：新型15元大环内酯衍生物的合成和抗菌活性：阿奇霉素的4''-氨基甲酸酯，11,12-环状碳酸酯-4''-氨基甲酸酯和11,4''-二-O-芳基氨基甲酰基类似物。
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 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。
4. Lewis Acid-Catalyzed Synthesis of Cyclic Carbamates from N-Boc- Protected Aminals and Alkynes [C] . Kento Yasumoto, Taichi Kano, Keiji Maruoka 日本化学会春季年会講演予稿集 . 2018

机译：Lewis酸催化的N- Boc-受芳基和炔烃的环状氨基甲酸酯的合成
5. Regioselective, Asymmetric α,α-Bisalkylation of Ketones via N-Amino Cyclic Carbamate Chiral Auxiliaries: Methodology Development and Application to the Total Synthesis of both (+)- and (-)-Stigmolone and Apratoxin D [D] . Wengryniuk, Sarah Elizabeth 2012

机译：通过N-氨基环状氨基甲酸酯手性助剂的酮的区域选择性，不对称α，α-双烷基化：方法学的发展和在（+）-和（-）-Stigmolone和Apratoxin D的总合成中的应用
6. Synthesis and Antibacterial Activity of a Novel Class of 15-Membered Macrolide Antibiotics 11a-Azalides [O] . Tomohiro Sugimoto, *, Tetsuya Tanikawa 2011

机译：一类新型的十五元大环内酯类抗生素 11a-氮杂内酯的合成与抑菌活性
7. Studies on the Synthesis of Antiulcer Agents. II. Synthesis and Antiulcer Activity of Cyclic Carbamate Derivatives [O] . MICHIHIRO KOBAYASHI, MAKIO KITAZAWA, TAKENAO SAITO, 1984

机译：抗腐蚀剂的合成研究。 II。环状氨基甲酸酯衍生物的合成及抗溃剂活性

Synthesis and antibacterial activity of novel 15-membered macrolide derivatives: 4''-carbamate, 11,12-cyclic carbonate-4''-carbamate and 11,4''-di-O-arylcarbamoyl analogs of azithromycin.

摘要

著录项

相似文献

相关主题

期刊订阅