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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. III. Optimization of a phenyl thiadiazole moiety
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Synthesis and antibacterial activity of novel lincomycin derivatives. III. Optimization of a phenyl thiadiazole moiety

机译:新型林核糖蛋白衍生物的合成及抗菌活性。 III。 优化苯基噻二唑部分

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摘要

Lincomycin derivatives that have a 5-(2-nitrophenyl)-1,3,4-thiadiazol-2-yl thio moiety at the 7-position were synthesized. 5-Substituted 2-nitrophenyl derivatives showed potent antibacterial activities against Streptococcus pneumoniae and Streptococcus pyogenes with erm gene. Antibacterial activities of the 4,5-di-substituted 2-nitrophenyl derivatives were generally comparable to those of telithromycin (TEL) against S. pneumoniae with erm gene and clearly superior to those of TEL against S. pyogenes with erm gene. Compounds 6 and 10c that have a methoxy group at the 5-position of the benzene ring exhibited activities comparable to TEL against Haemophilus influenzae. These results suggest that lincomycin derivatives modified at the 7-position would be promising compounds as a clinical candidate. We would like to dedicate this article to the special issue for late Professor Dr. Hamao Umezawa in The Journal of Antibiotics.
机译:合成含有5-(2-硝基苯基)-1,3,4-噻唑-2-基噻唑-2-基硫代噻唑-2-基硫代噻唑硫醚的延伸蛋白衍生物被合成了7-位。 5-取代的2-硝基苯基衍生物显示出与ERM基因的肺炎链球菌和链球菌化脓性的有效的抗菌活性。 4,5-二取代的2-硝基苯基衍生物的抗菌活性通常与具有ERM基因的汽油霉素(Tel)对抗S.肺炎的那些,并且明显优于与ERM基因的Tel对抗S. pyogenes的那些。 在苯环5位的化合物6和10C,在苯环的5-位表现出与Tel对抗嗜血杆菌嗜血杆菌的活性。 这些结果表明,在7位修饰的林霉素衍生物将是有前途的化合物作为临床候选者。 我们想将这篇文章致力于抗生素杂志Hameo Umezawa博士的特殊问题。

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