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异丙氧基苯胍具有杀菌作用且未发现耐药性。

Isopropoxy Benzene Guanidine Kills Without Detectable Resistance.

作者信息

Zhang Xiufeng, Xiong Wenguang, Peng Xianfeng, Lu Yixing, Hao Jie, Qin Zonghua, Zeng Zhenling

机构信息

National Risk Assessment Laboratory for Antimicrobial Resistance of Animal Original Bacteria, Guangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation, College of Veterinary Medicine, South China Agricultural University, Guangzhou, China.

Guangdong Laboratory for Lingnan Modern Agriculture, Guangzhou, China.

出版信息

Front Microbiol. 2021 Feb 4;12:633467. doi: 10.3389/fmicb.2021.633467. eCollection 2021.

Abstract

Serious infections caused by multidrug-resistant clearly urge the development of new antimicrobial agents. Drug repositioning has emerged as an alternative approach that enables us to rapidly identify effective drugs. We first reported a guanidine compound, isopropoxy benzene guanidine, had potent antibacterial activity against Unlike conventional antibiotics, repeated use of isopropoxy benzene guanidine had a lower probability of resistance section. We found that isopropoxy benzene guanidine triggered membrane damage by disrupting the cell membrane potential and cytoplasmic membrane integrity. Furthermore, we demonstrated that isopropoxy benzene guanidine is capable of treating invasive MRSA infections studies. These findings provided strong evidence that isopropoxy benzene guanidine represents a new chemical lead for novel antibacterial agent against multidrug-resistant infections.

摘要

由多重耐药菌引起的严重感染明显促使新型抗菌药物的研发。药物重新定位已成为一种替代方法,使我们能够快速识别有效药物。我们首次报道了一种胍类化合物,异丙氧基苯胍,对……具有强大的抗菌活性。与传统抗生素不同,重复使用异丙氧基苯胍产生耐药性的概率较低。我们发现异丙氧基苯胍通过破坏细胞膜电位和细胞质膜完整性引发膜损伤。此外,我们证明异丙氧基苯胍能够治疗侵袭性耐甲氧西林金黄色葡萄球菌感染……研究。这些发现提供了强有力的证据,表明异丙氧基苯胍是针对多重耐药菌感染的新型抗菌剂的一种新的化学先导物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd5f/7890237/2be65aefbff5/fmicb-12-633467-g001.jpg

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