新型1-[(2,4-(二叔丁基苯氧基))-3-二烷基氨基-2-丙醇]衍生物的抗菌活性

N. Vrynchanu, Yurii Korotkij, N. Hrynchuk, I. Boiko, E. Smertenko, L. Bondarenko
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引用次数: 0

摘要

介绍。微生物生物膜形成能力是新兴的抗生素耐药性问题的主要方面之一,这使得它们对抗生素和宿主防御系统以及其他外部压力具有耐受性,从而导致持续的慢性感染。一系列相关研究证实了氨基丙醇衍生物的高效抗菌和抗真菌作用。本研究旨在评价新型1-[(2,4-(二叔丁基苯氧基))-3-二烷基氨基-2-丙醇]衍生物对浮游细菌/真菌细胞和生物膜的抑菌活性。材料和方法。采用标准方法测定了新化合物的最低抑菌浓度(MIC),并通过龙胆紫吸附-解吸法测定了新化合物对生物膜的影响。КVM-219化合物对浮游细菌和真菌细胞的作用最为显著。不同菌株的MIC值在0.78 ~ 12.5 μg/mL之间。KVM-316化合物对生物膜的抑制作用最强,可阻止金黄色葡萄球菌(96.1%)、大肠杆菌(57.2%)和铜绿假单胞菌(96.1%)形成生物膜。结论。新合成的15个1-[(2,4-(二叔丁基苯氧基))-3-二烷基氨基-2-丙醇]衍生物对浮游微生物具有明显的抗菌和抗真菌作用。其中大多数化合物对金黄色葡萄球菌222、大肠杆菌311、铜绿假单胞菌449和光斑C. 404菌株的生物膜形成具有至少50%的抑制作用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Antimicrobial activity of novel 1-[(2,4-(di-tert-butylphenoxy))-3-dialkylamino-2-propanol] derivativesy
Introduction. The microbial biofilm-forming ability is one of the major aspects of the emerging issue of antibiotic resistance, which makes them tolerant to antibiotics and host defense systems and other external stresses, thus contributing to persistent chronic infections. A series of relevant studies confirmed the high efficiency of aminopropanol derivatives as potential antibacterial and antifungal agents. This present study was aimed to evaluate the antimicrobial activity of new 1-[(2,4-(di-tert-butylphenoxy))-3-dialkylamino-2-propanol] derivatives on the planktonic bacterial/fungal cells and biofilms. Material and methods. The minimum inhibitory concentrations (MIC) of the new compounds were determined by a standard method, along with their effects on biofilms estimated via the gentian violet adsorption-desorption assay.Results. The КVM-219 compound showed the most pronounced effect on planktonic bacterial and fungal cells. The MIC values ranged between 0.78 μg/mL to 12.5 μg/mL, depending on the microbial strain. The KVM-316 compound exhibited the strongest inhibitory effect on biofilms, thus preventing their formation by S. aureus (96.1%), E. coli (57.2%), and P. aeruginosa (96.1%). Conclusions. The 15 newly synthesized 1-[(2,4-(di-tert-butylphenoxy))-3-dialkylamino-2-propanol] derivatives revealed marked antibacterial and antifungal effects on planktonic microorganisms. Most of these compounds showed a strain-specific inhibition of biofilm formation by at least 50% for S. aureus 222, E. coli 311, P. aeruginosa 449 and C. glabrata 404 strains.
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