No abstract

The emergence and spread of resistant strains of pathogens as well as reduction of the efficacy of current antimicrobial agents requires the development of novel antimicrobial compounds. The aim of the present study was synthesis and evaluation of antimicrobial activity of new arylaliphatic aminopropanols. The objects of the present study were 1-[4-(1,1,3,3-tetramethylbutyl)phenoxy]-3-dialkylamino-2-propanol quaternary salts (compounds I–XIV). Compounds synthesis was carried out by heating of precursor epoxide and excessive amount of appropriate amines in isopropanole, followed by treatment with excess of alkyl halides. Methods of elemental analysis, IR- and PMR-spectroscopy were used for confirmation of chemical structure. Antimicrobial activity against Staphylococcus аureus АTCC 25923, Escherichia coli ATCC 25922, Pseudomonas aeruginosa АТСС 27853 and Candida albicans NCTC 885/653 was determined by a broth dilution method and evaluated via minimum inhibitory concentration (MIC). Our investigation of antibacterial and antifungal activity of 1-[4-(1,1,3,3-tetra methylbutyl)phenoxy]-3-dialkylamino-2-propanol quaternary salts showed that compounds possess narrow spectrum, as well as broad spectrum action. Significant antimicrobial activity of the novel aryl aliphatic aminoalcohols indicates their potential usage as a component of new antimicrobial drugs.

Мета роботи -дослідити антивірусну дію нових сполук амінопропанолу-2 до вірусу бичачої вірусної діареї (BVDV) та в експериментальній продукувальній моделі вірусу гепатиту С (HCV 1-трет-бутокси-3-(2,2,6,6-тетраметил-4-гідрокси-піпе-ридино)-2-пропанол (речовина 50

<p><em>Здійснено</em><em> </em><em>синтез</em><em>, </em><em>вивчено</em><em> </em><em>фізико</em><em>-</em><em>хімічні</em><em> </em><em>властивості</em><em> </em><em>та</em><em> </em><em>антимікробну</em><em> </em><em>активність</em><em> </em><em>четвертинних </em><em>солей</em><em> 1-[4-(1-</em><em>адамантил</em><em>)-</em><em>фенокси</em><em>]-3-</em><em>діалкіламіно</em><em>-2-</em><em>пропанолу</em><em>.</em></p>

Synthesis and biological activity of novel adamantane-based dialkylaminopropanol quaternary salts Topicality. The emergence and spread of multidrug-resistant pathogens leads to a decrease in efficacy of antibiotic therapy, causes the duration of patient's hospital stay and increases 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. Aim. To synthesize and to make 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. Materials and methods. The synthesis and investigation of physicochemical properties of new adamantane-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.