Abstract

The emergence and spread of multidrug-resistant pathogens leads to a decrease in efficacy of antibiotic therapy, prolongation of the length of patient’s hospital stay and an increase in treatment costs. The screening of potential antimicrobial agents among the new classes of chemical compounds is one of the promising methods to overcome the problem of resistance.Objectives. The synthesis and screening studies of antimicrobial activity of quaternary salts of adamantane derivatives (3a – 3l) with the aim to find of new prospective compound with good activityMaterials and methods. The synthesis and investigation of physicochemical properties of new adamantan-based dialkylaminopropanol quaternary salts were carried out. The evaluation of antimicrobial action against S. aureus, E. coli and C. albicans strains were performed.Results and discussion. The results showed that the inhibitory activities of quaternary salts with 1-adamantylethyl radical in their alkoxy group were significantly higher than those of the compounds with 1-adamantyl and 1-adamantyloxyethyl radicals in their alkoxy group.Conclusions. 3c was the most active compound tested against all strains, with MIC between 1.56 and 3.12 µg/mL, and its antimicrobial activity was similar to that of myramistin.

Highlights

  • Nowadays, the emergence and spread of multidrugresistant (MDR) pathogens (e.g. methicillin-resistant Staphylococcus aureus (MRSA), carbapenem-resistant Enterobacteriaceae (CRE), fluoroquinolone-resistant Escherichia coli or resistant to third-generation cephalosporins Neisseria gonorrhoeae isolates) pose a global threat to public health

  • The results showed that the inhibitory activities of quaternary salts with 1-adamantylethyl radical in their alkoxy group were significantly higher than those of the compounds with 1-adamantyl and 1-adamantyloxyethyl radicals in their alkoxy group

  • The aim is to carry out synthesis and screening studies of antimicrobial activity of quaternary salts of adamantane derivatives (3a-3l) with the aim to find of new prospective compound with good activity

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Summary

Introduction

The emergence and spread of multidrugresistant (MDR) pathogens (e.g. methicillin-resistant Staphylococcus aureus (MRSA), carbapenem-resistant Enterobacteriaceae (CRE), fluoroquinolone-resistant Escherichia coli or resistant to third-generation cephalosporins Neisseria gonorrhoeae isolates) pose a global threat to public health. According to WHO data about antibiotic-resistance (2014), the lethality in patients with MRSA infection is higher on 64 % than with susceptible form of infection [1]. A wide spread of MDR-pathogens leads to a decrease in efficacy of antibiotic therapy, prolongation of the length of patient’s hospital stay and an increase in treatment costs. The screening of potential antimicrobial agents among the new classes of chemical compounds is one of the promising methods to overcome the problem of resistance. In this respect, adamantane-based aminopropanols are attracting attention owing to their broad antibacterial and antifungal activity [2, 3]. The aim is to carry out synthesis and screening studies of antimicrobial activity of quaternary salts of adamantane derivatives (3a-3l) with the aim to find of new prospective compound with good activity

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