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生物-有机金属抗生素衍生物。

Bio-Organometallic Derivatives of Antibacterial Drugs.

机构信息

Departamento de Química Orgánica, Facultad de Química, Universidad Complutense, 28040, Madrid, Spain.

Centro de Innovación en Química Avanzada (ORFEO-CINQA), Facultad de Química, Universidad Complutense, 28040, Madrid, Spain.

出版信息

Chemistry. 2019 May 28;25(30):7232-7242. doi: 10.1002/chem.201805985. Epub 2019 Mar 18.

DOI:10.1002/chem.201805985
PMID:30730065
Abstract

Overuse and misuse of antibacterial drugs has resulted in bacteria resistance and in an increase in mortality rates due to bacterial infections. Therefore, there is an imperative necessity of new antibacterial drugs. Bio-organometallic derivatives of antibacterial agents offer an opportunity to discover new active antibacterial drugs. These compounds are well-characterized products and, in several examples, their antibacterial activities have been studied. Both inhibition of the antibacterial activity and strong increase in the antibiotic activity of the parent drug have been found. The synthesis of the main classes of bio-organometallic derivatives of these drugs, as well as examples of the use of structure-activity relation (SAR) studies to increase the activity and to understand the mode of action of bio-organometallic antimicrobial peptides (BOAMPs) and platensimicyn bio-organometallic mimics is presented in this article.

摘要

抗菌药物的过度使用和滥用导致了细菌耐药性的产生,并使细菌感染导致的死亡率上升。因此,我们迫切需要新的抗菌药物。抗菌药物的生物有机金属衍生物为发现新的有效抗菌药物提供了机会。这些化合物是特征明确的产品,并且在许多情况下,已经对它们的抗菌活性进行了研究。已经发现了对母体药物的抗菌活性的抑制和强烈的增强。本文介绍了这些药物的主要生物有机金属衍生物的合成,以及使用结构-活性关系(SAR)研究来提高活性和理解生物有机金属抗菌肽(BOAMPs)和platensimicyn 生物有机金属模拟物的作用模式的例子。

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Bio-Organometallic Derivatives of Antibacterial Drugs.生物-有机金属抗生素衍生物。
Chemistry. 2019 May 28;25(30):7232-7242. doi: 10.1002/chem.201805985. Epub 2019 Mar 18.
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[An old pathway to new antibiotics--platensimycin].[通往新型抗生素的一条老路——扁平霉素]
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Synthesis and antimicrobial evaluation of novel platensimycin analogues.新型盘菌霉素类似物的合成与抗菌评价。
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Platensimycin: a promising antimicrobial targeting fatty acid synthesis.普拉特烯霉素:一种有前景的靶向脂肪酸合成的抗菌药物。
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Dialkylamino-2,4-dihydroxybenzoic acids as easily synthesized analogues of platensimycin and platencin with comparable antibacterial properties.二烷基氨基-2,4-二羟基苯甲酸作为易于合成的藤黄紫霉素和藤黄绿菌素类似物,具有相当的抗菌特性。
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