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Design and Synthesis of Small Molecules as Potent Staphylococcus aureus Sortase A Inhibitors
Antibiotics ( IF 4.8 ) Pub Date : 2020-10-16 , DOI: 10.3390/antibiotics9100706
Min Woo Ha , Sung Wook Yi , Seung-Mann Paek

The widespread and uncontrollable emergence of antibiotic-resistant bacteria, especially methicillin-resistant Staphylococcus aureus, has promoted a wave of efforts to discover a new generation of antibiotics that prevent or treat bacterial infections neither as bactericides nor bacteriostats. Due to its crucial role in virulence and its nonessentiality in bacterial survival, sortase A has been considered as a great target for new antibiotics. Sortase A inhibitors have emerged as promising alternative antivirulence agents against bacteria. Herein, the structural and preparative aspects of some small synthetic organic compounds that block the pathogenic action of sortase A have been described.

中文翻译:

小分子强效金黄色葡萄球菌Sortase A抑制剂的设计与合成

抗生素耐药性细菌,尤其是耐甲氧西林金黄色葡萄球菌的广泛出现和不可控制的出现,推动了人们努力寻找一种新一代的抗生素,这些抗生素既可以预防也不能治疗细菌感染,而不能作为杀菌剂或抑菌剂。由于其在毒力中的关键作用及其在细菌存活中的重要性,分选酶A被认为是新抗生素的重要靶标。Sortase A抑制剂已成为有前途的替代细菌抗毒剂。在此,已经描述了一些阻止分选酶A的致病作用的小的合成有机化合物的结构和制备方面。
更新日期:2020-10-17
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