Abstract
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.
Highlights
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, contributing to persistent chronic infections
Bacterial strain and growth conditions The study was conducted on the gram-positive (Staphylococcus aureus subsp. aureus (ATCC® 25923TM), S. aureus 222 (MRSA)) and gram-negative (Escherichia coli (ATCC® 25922TM), E. coli 311, Pseudomonas aeruginosa (ATCC® 27853 TM), P. aeruginosa 449) bacterial strains, and yeasts (Candida albicans NTCC 885/653, C. glabrata 404)
The studies of antibacterial and antifungal activities confirmed that 1-[(2,4-(di-tert-butylphenoxy))-3-dialkylamino-2-propanol] new derivatives caused inhibitory effect on S. aureus and C. albicans, with the minimum inhibitory concentrations (MIC) values ranging from 0.78 to 3.75 μg/mL and from 1.56 to 20.0 μg/mL, respectively. These compounds revealed no antibacterial effects against gram-negative bacteria, except for the VII and IV compounds, the МІС value for E. coli reaching to 12.5 μg/mL and 20.0 μg/mL, respectively
Summary
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, contributing to persistent chronic infections. The goal of the global action plan is to ensure, for as long as possible, continuity of successful treatment and prevention of infectious diseases by effective and safe medicines that are quality-assured, used in a responsible way and accessible to all who need them To achieve this goal, five strategic objectives have been set out: to improve awareness and understanding of antimicrobial resistance; to strengthen knowledge through surveillance and research; to reduce the incidence of infection; to optimize the use of antimicrobial agents; to develop the economic case for sustainable investment that takes account of the needs of all countries; and to increase investments in new medicines, diagnostic tools, vaccines and other interventions [3]. Considering all of the above mentioned, the most promising approach is to search for potentially novel antimicrobial agents for combatting antimicrobial resistance
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