吡啶和嘧啶衍生物抗MRSA研究进展

Adarsh Kumar, Ankit Kumar Singh, Suresh Thareja, Pradeep Kumar
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引用次数: 3

摘要

耐甲氧西林金黄色葡萄球菌(MRSA)是一种革兰氏阳性菌株,其对现有抗生素的耐药性是全球研究人员关注的主要问题。革兰氏阳性感染,特别是在金黄色葡萄球菌分离株中传播的耐甲氧西林金黄色葡萄菌,从2009年的29%呈指数级增长到2014年的47%。文献综述显示,全球约13-74%的金黄色葡萄球菌菌株对甲氧西林具有耐药性。在这篇文章中,我们总结了细菌耐药性的机制,治疗MRSA的分子靶点,以及已报道的吡啶和嘧啶衍生物对耐甲氧西林金黄色葡萄球菌的活性。本研究收集的数据来自在线同行评审的研究文章和使用薛定谔软件的Maestro模块对已报道的抗MRSA药物进行的分子对接研究。计算机研究结果表明,一些吡啶衍生物比标准抗MRSA药物具有更好的结合相互作用。已报道的吡啶衍生物的分子对接研究为开发新型抗MRSA药物带来了极好的成功。总的来说,这项研究将对设计和开发基于靶点的抗MRSA药物的研究人员具有极其重要的意义。
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A review of pyridine and pyrimidine derivatives as anti-MRSA agents
Methicillin-resistant Staphylococcus aureus (MRSA) is a gram-positive strain whose resistance against existing antibiotics is a major concern for the researchers across the globe. Gram-positive infections, particularly methicillin-resistant Staphylococcus aureus spreading among S. aureus isolates, observed to increase exponentially from 29% in 2009 to 47% in 2014. Literature reviews revealed about 13-74% of worldwide S. aureus strains are Methicillin-resistant. In this article, we have summarized the mechanism of bacterium resistance, molecular targets to treat MRSA, and the activity of reported pyridine and pyrimidine derivatives against methicillin-resistant Staphylococcus aureus. The data collected for this study from online peer reviewed research articles and Molecular-docking study of reported anti-MRSA agents performed by using Maestro Module of Schrodinger software. Results of in silico studies showed that some pyridine derivatives having better binding interactions than standard anti-MRSA agents. Molecular docking studies of reported pyridine derivatives resulted in excellent hits for the development of novel anti- MRSA agents. Overall, this study will be immense importance for researchers working in design and development of target based anti-MRSA agents.
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来源期刊
Anti-Infective Agents
Anti-Infective Agents Pharmacology, Toxicology and Pharmaceutics-Pharmacology
CiteScore
1.50
自引率
0.00%
发文量
47
期刊介绍: Anti-Infective Agents publishes original research articles, full-length/mini reviews, drug clinical trial studies and guest edited issues on all the latest and outstanding developments on the medicinal chemistry, biology, pharmacology and use of anti-infective and anti-parasitic agents. The scope of the journal covers all pre-clinical and clinical research on antimicrobials, antibacterials, antiviral, antifungal, and antiparasitic agents. Anti-Infective Agents is an essential journal for all infectious disease researchers in industry, academia and the health services.
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