单阳离子和双阳离子吡啶并[1,2,4]恶二唑和三唑的合成及抗菌活性。

Synthesis and Antibacterial Activity of Mono- and Bi-Cationic Pyridinium 1,2,4-Oxadiazoles and Triazoles.

机构信息

Department of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Viale delle Scienze, Ed. 17, 90128 Palermo, Italy.

Department of Health Promotion, Mother and Child Care, Internal Medicine and Medical Specialties "G D'Alessandro", University of Palermo, Via Del Vespro 133, 90127 Palermo, Italy.

出版信息

Int J Mol Sci. 2023 Dec 27;25(1):377. doi: 10.3390/ijms25010377.

DOI:10.3390/ijms25010377

PMID:38203549

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10778652/

Abstract

One of the main causes of mortality in humans continues to be infectious diseases. Scientists are searching for new alternatives due to the fast increase in resistance of some harmful bacteria to the frontline antibiotics. To effectively treat pathogenic infections, it is crucial to design antibiotics that can prevent the development of pathogenic resistance. For this purpose, a set of 39 quaternary pyridinium and bis-pyridinium salts with different lengths of side alkyl or fluorinated chains, heterocyclic spacers, and counter ions were tested on diverse reference bacterial ATCC (American Type Culture Collection) strains, such as and . Subsequently, 6 out of the 39 pyridinium salts showing relevant MIC (Minimum Inhibitory Concentration) values were tested on clinically isolated, resistant strains of , , , , , and . Additional tests have been performed to assess if the minimum concentration detected through MIC assay may limit the growth of biofilms.

摘要

在人类死亡的主要原因中，传染病仍然是一个主要原因。由于一些有害细菌对一线抗生素的耐药性迅速增加，科学家们正在寻找新的替代品。为了有效治疗病原性感染，设计能够预防病原性耐药性发展的抗生素至关重要。为此，一组 39 种具有不同侧链烷基或氟化链长度、杂环间隔物和抗衡离子的季铵盐和双季铵盐对不同的参考细菌 ATCC（美国典型培养物保藏中心）菌株进行了测试，如和。随后，对 39 种季铵盐中的 6 种显示出相关 MIC（最小抑菌浓度）值的盐在临床上分离出的、耐药的、、、、和菌株上进行了测试。还进行了额外的测试，以评估 MIC 测定中检测到的最低浓度是否可能限制生物膜的生长。