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首页> 外文期刊>The Journal of Antibiotics: An International Journal >In vitro antibacterial activity of alpha-methoxyimino acylide derivatives against macrolide-resistant pathogens and mutation analysis in 23S rRNA
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In vitro antibacterial activity of alpha-methoxyimino acylide derivatives against macrolide-resistant pathogens and mutation analysis in 23S rRNA

机译：α-甲氧基亚氨基酰胺衍生物对大氯化物抗性病原体的体外抗菌活性和23s rRNA的突变分析

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摘要

We characterized in vitro activities of alpha-methoxyimino acylides against macrolide-resistant clinical isolates of Streptococcus pneumoniae, Streptococcus pyogenes and Mycoplasma pneumoniae with ribosome modification or substitution and selected acylide-resistant mutants to clarify the binding point of the acylides. The acylides had low MICs against erm(B) gene-containing S. pneumoniae and S. pyogenes (MIC(90)s, 1-4 mu g ml(-1)). For M. pneumoniae, although they had poor potencies against macrolide-resistant strains with the A2058G (Escherichia coli numbering) mutation in 23S rRNA (MICs, >32 mu g ml(-1)), one of them showed in vitro activities against macrolide-resistant strains with the A2058U or A2059G mutations (MICs, 0.5-1 mu g ml(-1)). These A2058U and A2059G mutant strains were used for the selection of acylide-resistant mutants. A genetic analysis showed that new point mutations in acylide-resistant mutants were found at G2576 in domain V of 23S rRNA and at Lys90 in L22 ribosomal protein. Furthermore, a molecular modeling study revealed that G2505/C2610, which enables stacking with G2576, might interact with a pyridyl moiety or an alpha-methoxyimino group at the 3-position of acylides. The cc-methoxyimino acylides were shown to possess a tertiary binding point at G2505/C2610 in 23S rRNA. Our results suggest that alpha-methoxyimino acylides represent significant progress in macrolide antimicrobials.
机译：我们以具有核糖体改性或取代和选定的酰胺突变体和选自酰胺突变体的α-甲氧基氨基氨基酰化物对α-甲氧基氨基氨基酰化物的体外活性，抗链球菌肺炎链球菌抗性临床分离物，并选择酰胺抗突变体。酰胺对含有ERM（B）基因的S.肺炎肺炎和S. pyogenes（MIC（90）S，1-4μg（-1））的低麦克白。对于M.肺炎，虽然它们对23s rRNA（MICS，>32μg（-1）中的A2058G（大肠杆菌Coli编号）突变具有较差的抗大氯化物抗性菌株抗性株（MICS，>32μg（-1）），但其中一项对大环内酯进行体外活性 - 使用A2058U或A2059G突变（MICS，0.5-10mg mL（-1））的菌株。这些A2058U和A2059G突变菌株用于选择抗酰胺突变体。遗传分析表明，在L22核糖体蛋白蛋白蛋白蛋白蛋白蛋白蛋白蛋白的域V23S v中的G2576中发现了偶氮抗突变体中的新点突变。此外，分子建模研究表明，能够用G2576堆叠的G2505 / C2610可以与酰基酰胺的3-位的吡啶基部分或α-甲氧基咪唑相互作用。显示CC-甲氧基氨基酰基酰化物在23s rRNA中具有在G2505 / C2610的第三末结合点。我们的研究结果表明，α-甲氧基咪唑酯酰胺在大环内德抗微生物中具有显着进展。

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