Department of Pharmaceutical Chemistry, Faculty of Pharmacy, "Carol Davila" University of Medicine and Pharmacy, 6 Traian Vuia, 020956 Bucharest, Romania.
Department of Pharmaceutical Botany, Faculty of Pharmacy, "Carol Davila" University of Medicine and Pharmacy, 6 Traian Vuia, 020956 Bucharest, Romania.
Molecules. 2021 May 18;26(10):3002. doi: 10.3390/molecules26103002.
Antimicrobial resistance is one of the major public health threats at the global level, urging the search for new antimicrobial molecules. The fluorene nucleus is a component of different bioactive compounds, exhibiting diverse pharmacological actions. The present work describes the synthesis, chemical structure elucidation, and bioactivity of new O-aryl-carbamoyl-oxymino-fluorene derivatives and the contribution of iron oxide nanoparticles to enhance the desired biological activity. The antimicrobial activity assessed against three bacterial and fungal strains, in suspension and biofilm growth state, using a quantitative assay, revealed that the nature of substituents on the aryl moiety are determinant for both the spectrum and intensity of the inhibitory effect. The electron-withdrawing inductive effect of chlorine atoms enhanced the activity against planktonic and adhered , while the +I effect of the methyl group enhanced the anti-fungal activity against strain. The magnetite nanoparticles have substantially improved the antimicrobial activity of the new compounds against planktonic microorganisms. The obtained compounds, as well as the magnetic core@shell nanostructures loaded with these compounds have a promising potential for the development of novel antimicrobial strategies.
抗菌耐药性是全球范围内主要的公共卫生威胁之一，促使人们寻找新的抗菌分子。芴核是不同生物活性化合物的组成部分，表现出多种药理作用。本工作描述了新型 O-芳基氨基甲酰氧基-芴衍生物的合成、化学结构阐明和生物活性，以及氧化铁纳米粒子对增强所需生物活性的贡献。使用定量测定法评估了这些化合物对三种细菌和真菌菌株在悬浮和生物膜生长状态下的抗菌活性，结果表明芳基部分取代基的性质对抑制作用的谱和强度都有决定性的影响。氯原子的吸电子诱导效应增强了对浮游生物和附着生物的活性，而甲基的+I 效应增强了对 菌株的抗真菌活性。磁铁矿纳米粒子大大提高了这些新型化合物对浮游微生物的抗菌活性。所获得的化合物以及负载这些化合物的磁性核壳纳米结构具有开发新型抗菌策略的巨大潜力。
