支链肽：吖啶和硼酸衍生物作为抗菌剂
Branched Peptides: Acridine and Boronic Acid Derivatives as Antimicrobial Agents.
作者信息
Wynn Jessica E, Zhang Wenyu, Falkinham Joseph O, Santos Webster L
机构信息
Department of Chemistry, Virginia Tech, Blacksburg, Virginia 24061, United States.
Department of Biological Sciences, Virginia Tech, Blacksburg, Virginia 24061, United States.
出版信息
ACS Med Chem Lett. 2017 Jul 12;8(8):820-823. doi: 10.1021/acsmedchemlett.7b00119. eCollection 2017 Aug 10.
Abstract
The emergence of microbial resistance presents a challenge in the development of next generation therapeutics. Herein, we report the discovery of branched peptides decorated with acridine and boronic acid moieties with potent antimicrobial activity. The results revealed minimal inhibitory concentrations (MICs) as low as 1 μg/mL against , , and . These peptides were nonhemolytic, and significantly inhibited growth of in suspension and biofilm formation. Structure-activity relationship studies suggest the acridine functional group as a driving force for the potent inhibition observed against bacteria.
摘要
微生物耐药性的出现给下一代治疗药物的开发带来了挑战。在此，我们报告了发现带有吖啶和硼酸部分修饰的具有强大抗菌活性的支链肽。结果显示，对[具体细菌名称1]、[具体细菌名称2]和[具体细菌名称3]的最低抑菌浓度（MIC）低至1μg/mL。这些肽无溶血作用，并能显著抑制[具体细菌名称]在悬浮液中的生长和生物膜形成。构效关系研究表明，吖啶官能团是观察到的对细菌有效抑制作用的驱动力。
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