Antimicrobial activity of novel 1-[(2,4-(di-tert-butylphenoxy))-3-dialkylamino-2-propanol] derivatives
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VRYNCHANU, Nina, KOROTKYI, Yurii, HRYNCHUK, Nataliia, BOIKO, Iryna, SMERTENKO, Elena, BONDARENKO, Larisa. Antimicrobial activity of novel 1-[(2,4-(di-tert-butylphenoxy))-3-dialkylamino-2-propanol] derivatives. In: One Health and Risk Management, 2021, nr. 2(3), pp. 27-33. ISSN 2587-3458. DOI: https://doi.org/10.38045/ohrm.2021.3.04
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One Health and Risk Management
Numărul 2(3) / 2021 / ISSN 2587-3458 /ISSNe 2587-3466

Antimicrobial activity of novel 1-[(2,4-(di-tert-butylphenoxy))-3-dialkylamino-2-propanol] derivatives

Activitatea antimicrobiană a noilor derivați de 1 - [(2,4-(di-tert-butylphenoxy)) - 3-dialkilamino-2-propanol]

DOI:https://doi.org/10.38045/ohrm.2021.3.04
CZU: 579.61:547.435+615.281

Pag. 27-33

Vrynchanu Nina1, Korotkyi Yurii2, Hrynchuk Nataliia1, Boiko Iryna1, Smertenko Elena2, Bondarenko Larisa1
 
1 Institute of Pharmacology and Toxicology, National Academy of Medical Sciences, Kiev,
2 Institute of Organic Chemistry NAS of Ukraine
 
 
Disponibil în IBN: 18 iunie 2021


Rezumat

Introduction. The microbial biofilm-forming ability is one of the major aspects of the emerg-ing 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 antimicro-bial 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 mi-croorganisms. Most of these compounds showed a strain-specific inhibition of biofilm for-mation by at least 50% for S. aureus 222, E. coli 311, P. aeruginosa 449 and C. glabrata 404 strains.

Introducere. Scopul studiului l-a constituit evaluarea efectelor antimicrobiene ale derivaților 1 - [(2,4 (di-terț- butylphenoxy)) - 3- dialkylamino-2-propanol] asupra celulelor planctonice bacteriene/fungice și asupra biofilmelor. Material și metode. Concentrațiile minime inhibitorii (CMI) ale compușilor noi au fost deter-minate printr-o metodă standard, activitatea antibiofilm a fost testată prin absorbția violetu-lui de gențiană pe structuri formate pe plăci de polistiren, urmată de resolubilizare cu solvent organic și resazurină ca indicator redox. Rezultate. Efectul cel mai pronunțat asupra celulelor planctonice bacteriene și fungice l-a demonstrat compusul КVM -219, CMI 0,67 μg/ml - 12,5 μg/ml, în funcție de microorganism, iar asupra biofilmelor - compusul KVM-316. KVM-316 a prevenit formarea biofilmelor de către S. aureus (96,1%), E. coli (57,2%) și P. aeruginosa (96,1%). Concluzii. Cei 15 derivați nou sintetizați ai 1 - [(2,4- (di- tert-butylphenoxy)) - 3- dialkylamino -2-propanol] au prezentat efecte antibacteriene și antifungice pronunțate asupra microorga-nismelor planctonice. Majoritatea acestor compuși au inhibat în mod specific formarea bio-filmelor de către tulpinile clinice S. aureus 222, E. coli 311, P. aeruginosa 449 și C. glabrata 404 cu cel puțin 50%.

Cuvinte-cheie
amino-propanol deriva-tives, antimicro-bial activity, bacte-ria, biofilm,

derivați de amino-propanol, activitate antimicro-biană, Bacterii, biofilm