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NHC-银配合物作为抗菌剂的结构-活性关系。

Structure-Activity Relationships in NHC-Silver Complexes as Antimicrobial Agents.

机构信息

Institut des Sciences Analytiques et de Physico-Chimie Pour l'Environnement et les Matériaux, Université de Pau et des Pays de l'Adour, E2S UPPA, CNRS, IPREM, 64053 Pau, France.

Department of Biology, University of Naples "Federico II", Via Cynthia, 80143 Naples, Italy.

出版信息

Molecules. 2023 May 30;28(11):4435. doi: 10.3390/molecules28114435.

Abstract

Silver has a long history of antimicrobial activity and received an increasing interest in last decades owing to the rise in antimicrobial resistance. The major drawback is the limited duration of its antimicrobial activity. The broad-spectrum silver containing antimicrobial agents are well represented by N-heterocyclic carbenes (NHCs) silver complexes. Due to their stability, this class of complexes can release the active Ag cations in prolonged time. Moreover, the properties of NHC can be tuned introducing alkyl moieties on N-heterocycle to provide a range of versatile structures with different stability and lipophilicity. This review presents designed Ag complexes and their biological activity against Gram-positive, Gram-negative bacteria and fungal strains. In particular, the structure-activity relationships underlining the major requirements to increase the capability to induce microorganism death are highlighted here. Moreover, some examples of encapsulation of silver-NHC complexes in polymer-based supramolecular aggregates are reported. The targeted delivery of silver complexes to the infected sites will be the most promising goal for the future.

摘要

银具有悠久的抗菌活性历史,由于抗菌耐药性的增加,近年来受到越来越多的关注。其主要缺点是抗菌活性的持续时间有限。含银的广谱抗菌剂主要由 N-杂环卡宾(NHCs)银配合物组成。由于其稳定性,这类配合物可以在长时间内释放出活性 Ag 阳离子。此外,通过在 N-杂环上引入烷基部分,可以调节 NHC 的性质,提供一系列具有不同稳定性和亲脂性的多功能结构。本综述介绍了设计的 Ag 配合物及其对革兰氏阳性、革兰氏阴性细菌和真菌菌株的生物活性。特别是,强调了突出增加诱导微生物死亡能力的主要要求的结构-活性关系。此外,还报告了将银-NHC 配合物包封在基于聚合物的超分子聚集体中的一些例子。将银配合物靶向递送至感染部位将是未来最有前途的目标。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/128b/10254942/ed6450e25b9c/molecules-28-04435-g003.jpg

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