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小分子碳水化合物衍生物作为有效的抗生物膜剂。

Small Carbohydrate Derivatives as Potent Antibiofilm Agents.

机构信息

Department of Chemistry, Indian Institute of Technology Bombay, Mumbai, India 400076.

出版信息

J Med Chem. 2022 Jul 14;65(13):8525-8549. doi: 10.1021/acs.jmedchem.1c01039. Epub 2022 Jul 1.

Abstract

Biofilm formation by most pathogenic bacteria is considered as one of the key mechanisms associated with virulence and antibiotic resistance. Biofilm-forming bacteria adhere to the surfaces of biological or implant medical devices and create communities within their self-produced extracellular matrix that are difficult to treat by existing antibiotics. There is an urgent need to synthesize and screen structurally diverse molecules for their antibiofilm activity that can remove or minimize the bacterial biofilm. The development of carbohydrate-based small molecules as antibiofilm agents holds a great promise in addressing the problem of the eradication of biofilm-related infections. Owing to their structural diversity and specificity, the sugar scaffolds are valuable entities for developing antibiofilm agents. In this perspective, we discuss the literature pertaining to carbohydrate-based natural antibiofilm agents and provide an overview of the design, activity, and mode of action of potent synthetic carbohydrate-based molecules.

摘要

生物膜的形成被大多数病原菌视为与其毒力和抗生素耐药性相关的关键机制之一。形成生物膜的细菌附着在生物或植入式医疗设备的表面,并在其自身产生的细胞外基质中形成群落,这些群落很难用现有的抗生素进行治疗。因此,迫切需要合成和筛选具有结构多样性的分子,以研究其抗生物膜活性,从而去除或最小化细菌生物膜。基于碳水化合物的小分子作为抗生物膜剂的发展在解决生物膜相关感染的根除问题方面具有巨大的潜力。由于其结构多样性和特异性,糖支架是开发抗生物膜剂的有价值实体。在这篇观点文章中,我们讨论了基于碳水化合物的天然抗生物膜剂的文献,并概述了有效合成基于碳水化合物的分子的设计、活性和作用模式。

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