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The intriguing biology and chemistry of fosfomycin: the only marketed phosphonate antibiotic

机译：福斯福霉素的有趣生物学和化学性：唯一的批次膦酸抗生素

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Recently infectious diseases caused by the increased emergence and rapid spread of drug-resistant bacterial isolates have been one of the main threats to global public health because of a marked surge in both morbidity and mortality. The only phosphonate antibiotic in the clinic, fosfomycin, is a small broad-spectrum molecule that effectively inhibits the initial step in peptidoglycan biosynthesis by blocking the enzyme, MurA in both Gram-positive and Gram-negative bacteria. As fosfomycin has a novel mechanism of action, low toxicity, a broad spectrum of antibacterial activity, excellent pharmacodynamic/pharmacokinetic properties, and good bioavailability, it has been approved for clinical use in the treatment of urinary tract bacterial infections in many countries for several decades. Furthermore, its potential use for difficult-to-treat bacterial infections has become promising, and fosfomycin has become an ideal candidate for the effective treatment of bacterial infections caused by multidrug-resistant isolates, especially in combination with other therapeutic drugs. Here we aim to present an overview of the biology and chemistry of fosfomycin including isolation and characterization, pharmacology, biosynthesis and chemical synthesis since its discovery in order to not only help scientists reassess the role of this exciting drug in fighting antibiotic resistance but also build the stage for discovering more novel phosphonate antibiotics in the future.
机译：最近由耐药细菌分离株的增加和迅速传播引起的传染病是全球公共卫生的主要威胁之一，因为发病率和死亡率显着飙升。临床磷酸含量在临床中，FOSFOMYCIN是一种小的宽谱分子，可通过阻断酶，植物在革兰氏阳性和革兰氏阴性细菌中有效地抑制肽聚糖生物合成的初始步骤。由于FOSFOMYCIN具有新的作用机制，低毒性，广泛的抗菌活性，优异的药物动力学/药代动力学性质以及良好的生物利用度，它已被批准用于治疗许多国家尿道细菌感染的临床用途几十年。此外，其对难以治疗的细菌感染的潜在用途已经有望，福斯福霉素已成为有效治疗由多药隔离物引起的细菌感染的理想候选者，特别是与其他治疗药物组合。在这里，我们旨在概述福斯福霉素的生物学和化学，包括分离和表征，药理学，生物合成和化学合成，因为它发现，以帮助科学家重新评估这种令人兴奋的药物在抗生素抗性中的作用，还可以建立在未来发现更多新型膦酸抗生素的阶段。

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    《RSC Advances》 |2019年第72期|共15页
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  • 中图分类 化学;
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