Synthesis and biological activity of novel adamantan-based dialkylaminopropanol quaternary salts

Authors

DOI:

https://doi.org/10.24959/ubphj.18.179

Keywords:

adamantane derivatives, dialkylaminopropanol, synthesis, antibacterial activity, antifungal action.

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 (3a3l) with the aim to find of new prospective compound with good activity

Materials 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.

References

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Korotkii, Y. V., Vrynchanu, N. A., Maksimov, Y. N., Lozinskii, M. O. (2011). Synthesis, antimicrobial and antifungal activities of quaternary salts of adamantane-containing alkoxydialkyl aminopropanols. Khimiko-farmatsevtichesky zhurnal – Pharmaceutical Chemistry Journal, 45(1), 21-23.

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Published

2018-08-20

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Section

Pharmaceutical chemistry and pharmacognosy