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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Synthesis and antibacterial activity of novel lincomycin derivatives. IV. Optimization of an N-6 substituent
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Synthesis and antibacterial activity of novel lincomycin derivatives. IV. Optimization of an N-6 substituent

机译：新型林核糖蛋白衍生物的合成及抗菌活性。 IV。 优化N-6取代基

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摘要

The design and synthesis of lincomycin derivatives modified at the C-6 and C-7 positions are described. A substituent at the C-7 position is a 5-aryl-1,3,4-thiadiazol-2-yl-thio group that generates antibacterial activities against macrolide-resistant Streptococcus pneumoniae and Streptococcus pyogenes carrying an erm gene. An additional modification at the C-6 position was explored in application of information regarding pirlimycin and other related compounds. These dual modifications were accomplished by using methyl alpha-thiolincosaminide as a starting material. As a result of these dual modifications, the antibacterial activities were improved compared with those of compounds with a single modification at the C-7 position. The antibacterial activities of selected compounds in this report against macrolide-resistant S. pneumoniae and S. pyogenes with an erm gene were superior to those of telithromycin.
机译：描述了在C-6和C-7位置修饰的林霉素衍生物的设计和合成。 C-7位置的取代基是5-芳基-1,3,4-噻二唑-2-基硫基醇基，产生针对耐受ERM基因的大氯化物抗性链球菌和链球菌化脓性的抗菌活性。 在应用关于皮坡蛋白和其他相关化合物的信息的应用中探讨了C-6位置的额外修改。 通过使用甲基α-硫氨胺胺作为原料来完成这些双重修饰。 由于这些双重修饰，与在C-7位置的单一改性的化合物相比，改善了抗菌活性。 本报告中所选化合物对大氯化物抗性S.肺炎的抗菌活性与ERM基因的肺炎肺炎氏菌素和S. pyogenes均优于汽霉素。

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