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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Synthesis and evaluation of biological activity of benzoxaborole derivatives of azithromycin
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Synthesis and evaluation of biological activity of benzoxaborole derivatives of azithromycin

机译：二十霉素苯并氧杂烯衍生物生物活性的合成与评价

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摘要

Novel benzoxaborole derivatives of azithromycin in which benzoxaborole residue is attached to the 4 ''-hydroxy-group of azithromycin have been synthesized. Antibacterial activity of synthesized derivatives in comparison with azithromycin was tested on a panel of Gram-positive and Gram-negative bacterial strains. All the investigated compounds demonstrated broad spectrum of antibacterial activity being in general more active against Gram-positive strains. New benzoxaborole derivatives of azithromycin demonstrated high activity against Streptococcus pyogenes ATCC 19615 and Propionibacterium acnes ATCC 6919 strains. Some of the new compounds were more active than azithromycin against Streptococcus pneumoniae ATCC 49619 strain or Enterococcus faecium strains. Using a reporter construct created on the basis of the transcription attenuator region of the Escherichia coli tryptophan operon pRFPCER-TrpL2A it has been demonstrated that the mechanism of action of azithromycin analogs is blocking nascent peptide in ribosome tunnel.
机译：合成了二十羟基霉素的新型苯并毒素衍生物，其中苯并氧杂烯残基附着于4'' - 羟基霉素中的羟基霉素。在革兰氏阳性和革兰氏阴性细菌菌群面板上测试了合成衍生物的合成衍生物的抗菌活性。所有研究的化合物都显示出广谱的抗菌活性，通常对革兰氏阳性菌株更加活跃。氮霉素的新苯并氧基硼衍生物展示了抗链球菌的高活性19615，抗菌剂ATCC 4919菌株。一些新化合物比阿奇霉素对肺炎链球菌ATCC 49619菌株或肠球菌粪便菌株更活跃。使用基于大肠杆菌色氨酸术术术术PRFPCER-TRPL2A的转录衰减器区域产生的报告构建体，已经证明了氮霉素类似物的作用机制阻断了核糖体隧道中的掺入肽。

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