Structure-Activity Relationships of Daptomycin Lipopeptides.,Journal of Medicinal Chemistry

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Structure-Activity Relationships of Daptomycin Lipopeptides.
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2020-07-20 , DOI: 10.1021/acs.jmedchem.0c00780
John A Karas ₁ , Glen P Carter ₂ , Benjamin P Howden ₂ , Adrianna M Turner ₂ , Olivia K A Paulin ₁ , James D Swarbrick ₁ , Mark A Baker ₃ , Jian Li ₄ , Tony Velkov ₁

Affiliation

Daptomycin is a calcium-dependent cyclic lipodepsipeptide derived from the soil saprotroph Streptomyces roseosporus, and its antibiotic properties make it a key agent for treatment of drug-resistant Gram-positive infections. It is most commonly used clinically for the treatment of Gram-positive skin and skin structure infections (SSSI), Staphylococcus aureus bacteremia, and right-sided endocarditis infections associated with S. aureus, including methicillin resistant S. aureus (MRSA). It has also been used “off-label” for Enterococcal infections. There has been a tremendous amount of research investigating its mode of action, resistance mechanisms, and biosynthesis of this clinically important antimicrobial agent. Although we cover the latter aspects in detail, the primary focus of this review is to provide the most comprehensive and up-to-date reference for the medicinal chemist on the structure–activity–toxicity of this important class of lipopeptide antibiotics.

中文翻译：

达托霉素脂肽的结构-活性关系。

达托霉素是源自土壤腐生玫瑰链霉菌的钙依赖性环脂肽，其抗生素特性使其成为治疗耐药革兰氏阳性感染的关键药物。它最常用于临床革兰氏阳性的治疗皮肤和皮肤结构感染（SSSI），金黄色葡萄球菌菌血症，并用相关的右侧心内膜炎的感染金黄色葡萄球菌，甲氧西林包括抗金黄色葡萄球菌（MRSA）。它还已被“标签外”用于肠球菌感染。有大量的研究对其作用模式，耐药机制以及这种临床上重要的抗菌剂的生物合成进行了研究。尽管我们详细介绍了后者，但本综述的主要重点是就这一重要的脂肽类抗生素的结构，活性和毒性为药物化学家提供最全面和最新的参考。

更新日期：2020-07-20

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