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超分子自缔合两亲物抑制关键病原体和的生物膜形成。

Supramolecular Self-Associating Amphiphiles Inhibit Biofilm Formation by the Critical Pathogens, and .

作者信息

Steyn Hendrik J F, White Lisa J, Hilton Kira L F, Hiscock Jennifer R, Pohl Carolina H

机构信息

Department of Microbiology and Biochemistry, University of the Free State, Bloemfontein, Free State 9301, South Africa.

School of Chemistry and Forensic Science, University of Kent, Kent, Canterbury CT2 7NH, United Kingdom.

出版信息

ACS Omega. 2023 Dec 22;9(1):1770-1785. doi: 10.1021/acsomega.3c08425. eCollection 2024 Jan 9.

Abstract

In 2019, 4.95 million deaths were directly attributed to antimicrobial-resistant bacterial infections globally. In addition, the mortality associated with fungal infections is estimated at 1.7 million annually, with many of these deaths attributed to species that are no longer susceptible to traditional therapeutic regimes. Herein, we demonstrate the use of a novel class of supramolecular self-associating amphiphilic (SSA) salts as antimicrobial agents against the critical pathogens and . We also identify preliminary structure-activity relationships for this class of compound that will aid the development of next-generation SSAs demonstrating enhanced antibiofilm activity. To gain insight into the possible mode of action for these agents, a series of microscopy studies were performed, taking advantage of the intrinsic fluorescent nature of benzothiazole-substituted SSAs. Analysis of these data showed that the SSAs interact with the cell surface and that a benzothiazole-containing SSA inhibits hyphal formation by .

摘要

2019年,全球有495万人的死亡直接归因于对抗菌素耐药的细菌感染。此外,与真菌感染相关的死亡率估计每年为170万,其中许多死亡归因于对传统治疗方案不再敏感的菌种。在此,我们展示了一类新型的超分子自缔合两亲(SSA)盐作为针对关键病原体和的抗菌剂的用途。我们还确定了这类化合物的初步构效关系,这将有助于开发具有增强抗生物膜活性的下一代SSA。为了深入了解这些药剂可能的作用方式,利用苯并噻唑取代的SSA的固有荧光性质进行了一系列显微镜研究。对这些数据的分析表明,SSA与细胞表面相互作用,并且含苯并噻唑的SSA抑制的菌丝形成。

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