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用于对抗耐甲氧西林金黄色葡萄球菌的革兰氏特异性抗菌咪唑四聚体的合理设计

Rational Design of Gram-Specific Antimicrobial Imidazolium Tetramers To Combat MRSA.

作者信息

Yuan Yuan, Shi Weiwei, Li Ruihua, Lim Diane S W, Armugam Arunmozhiarasi, Zhang Yugen

机构信息

Institute of Bioengineering and Nanotechnology, 31 Biopolis Way, The Nanos #04-01, Singapore 138669, Singapore.

2nd Hospital of Dalian Medical University, Dalian 116023, China.

出版信息

ACS Biomater Sci Eng. 2020 Oct 12;6(10):5563-5570. doi: 10.1021/acsbiomaterials.0c01248. Epub 2020 Sep 28.

Abstract

Antimicrobial resistance poses an increasingly serious global health threat. Hence, new antimicrobials with low propensity toward inducing resistance in bacteria are being developed to combat this threat. In this work, a series of imidazolium tetramers have been synthesized by modulating the linkers between imidazoliums or the length of the end groups within the structures of oligomers in order to optimize the activity, selectivity, and biocompatibility of the compounds. These new materials possess high biocompatibility, Gram selectivity, and high efficacy against the selected bacterium as well as clinically isolated methicillin-resistant species without inducing drug resistance. Therefore, we believe that these compounds can potentially be used to mitigate resistance as highly effective disinfectants in healthcare products or as antimicrobial therapies specifically for Gram-positive bacterial infections.

摘要

抗菌耐药性对全球健康构成了日益严重的威胁。因此,人们正在研发对细菌诱导耐药性倾向较低的新型抗菌药物来应对这一威胁。在这项工作中,通过调节咪唑鎓之间的连接基或低聚物结构中末端基团的长度,合成了一系列咪唑鎓四聚体,以优化化合物的活性、选择性和生物相容性。这些新材料具有高生物相容性、革兰氏选择性,对所选细菌以及临床分离的耐甲氧西林菌株具有高效性,且不会诱导耐药性。因此,我们认为这些化合物有可能作为医疗保健产品中的高效消毒剂或专门用于革兰氏阳性细菌感染的抗菌疗法来减轻耐药性。

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