Design, synthesis, and antibacterial evaluation of novel derivatives of NPS-2143 for the treatment of methicillin-resistant S. aureus (MRSA) infection.,The Journal of Antibiotics

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Design, synthesis, and antibacterial evaluation of novel derivatives of NPS-2143 for the treatment of methicillin-resistant S. aureus (MRSA) infection.
The Journal of Antibiotics ( IF 2.1 ) Pub Date : 2019-04-02 , DOI: 10.1038/s41429-019-0177-9
Yao Chen ₁ , Yuan Ju ₂ , Chungen Li ₂ , Tao Yang ₂ , Yong Deng ₁ , Youfu Luo ₂

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Methicillin-resistant Staphylococcus aureus (MRSA) infections are a significant global health challenge due to the emergence of strains exhibiting resistance to nearly all classes of antibiotics. This necessitates the rapid development of novel antimicrobials to circumvent this critical problem. Screening of compounds based on phenotypes is one of the major strategies for finding new antibiotics at present. Hence, we here performed a phenotypic screening against MRSA and identified NPS-2143 exhibiting activity against MRSA with an MIC value of 16 μg ml-1. In order to discover more potent anti-MRSA agents, a series of derivatives of NPS-2143 were designed and synthesized. The most promising compounds 48 and 49 exhibited favorable antimicrobial activity with an MIC value of 2 μg ml-1.

中文翻译：

NPS-2143新型衍生物用于耐甲氧西林金黄色葡萄球菌（MRSA）感染的设计，合成和抗菌评估。

耐甲氧西林金黄色葡萄球菌（MRSA）感染是对全球健康的重大挑战，因为出现了对几乎所有类型的抗生素都表现出抗药性的菌株。这就需要快速开发新型抗微生物剂来解决这一关键问题。基于表型的化合物筛选是目前寻找新抗生素的主要策略之一。因此，我们在这里针对MRSA进行了表型筛选，并确定了NPS-2143对MRSA表现出活性，其MIC值为16μgml-1。为了发现更有效的抗MRSA药物，设计并合成了一系列NPS-2143衍生物。最有前途的化合物48和49表现出良好的抗菌活性，MIC值为2μgml-1。

更新日期：2019-05-16

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