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卤代3-硝基-2-色烯作为抗多重耐药菌的潜在药物

Halogenated 3-Nitro-2-Chromenes as Potential Agents Against Multidrug-Resistant Bacteria.

作者信息

Godinho Patrícia I C, Pérez-Ramos Paula, Gabasa Yaiza, Cornielle Enmanuel, Soto Sara M, Soengas Raquel G, Silva Artur M S

机构信息

LAQV-REQUIMTE, Department of Chemistry, University of Aveiro, 3810-193 Aveiro, Portugal.

Department of Organic and Inorganic Chemistry, University of Oviedo, and Instituto Universitario de Química Organometálica Enrique Moles, C/Julián Clavería 8, 33006 Oviedo, Spain.

出版信息

Antibiotics (Basel). 2025 Feb 21;14(3):218. doi: 10.3390/antibiotics14030218.

Abstract

: Nosocomial infections caused by and resistant strains are an important cause of morbidity and mortality worldwide. Due to the increasing rate of resistance to conventional antibiotics, the discovery of new antibiotic drugs is crucial to keep pace with the evolution of these pathogenic bacterial species. : The 3-nitro-2-chromene moiety is present in several compounds with potent antibacterial activity; based on these previous studies, we report herein the synthesis of 20 new 2-aryl-3-nitro-2-chromene derivatives and the evaluation of their antibacterial potential in vitro. : Mono-halogenated nitrochromenes showed moderate anti-staphylococcal activity with MIC values of 8-32 μg/mL, whereas tri-halogenated 3-nitro-2-chromenes displayed potent anti-staphylococcal activities with MIC values of 1-8 μg/mL. Notably, 2-(4-bromophenyl)-6-bromo-8-chloro-3-nitro-2-chromene was the best antibacterial agent in the series against multidrug-resistant strains of and with MIC values of 4 μg/mL and 1-4 μg/mL, respectively. : nitrochromene shows a good safety profile, so it can be considered as a lead for further development.

摘要

由[具体细菌名称]和耐药菌株引起的医院感染是全球发病和死亡的重要原因。由于对传统抗生素的耐药率不断上升,发现新的抗生素药物对于跟上这些致病细菌物种的进化至关重要。:3-硝基-2-色烯部分存在于几种具有强大抗菌活性的化合物中;基于这些先前的研究,我们在此报告20种新的2-芳基-3-硝基-2-色烯衍生物的合成及其体外抗菌潜力的评估。:单卤代硝基色烯显示出中等的抗葡萄球菌活性,MIC值为8-32μg/mL,而三卤代3-硝基-2-色烯表现出强大的抗葡萄球菌活性,MIC值为1-8μg/mL。值得注意的是,2-(4-溴苯基)-6-溴-8-氯-3-硝基-2-色烯是该系列中对抗[具体细菌名称]和[具体细菌名称]多药耐药菌株的最佳抗菌剂,MIC值分别为4μg/mL和1-4μg/mL。:硝基色烯显示出良好的安全性,因此可被视为进一步开发的先导物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b620/11939745/169e8232ef85/antibiotics-14-00218-g001.jpg

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