The effect of substituents in the molecules of N-, R-alkyl amines on some gram-positive strains of microorganisms

M Yu Golik,S G Leonova,M A Komissarenko,T P Osolodchenko

doi:10.24959/nphj.15.2062

Abstract

The intensive use of antibiotics in patient care institutions often without determining specificity and sensitivity to them leads to more rapid development of resistance to pathogens of nosocomial infections; that is why it is one of the urgent problems of healthcare of Ukraine. The most common gram-positive pathogens of nosocomial infections are Staphylococcus aureus, coagulase-negative staphylococci and enterococci. In order to determine dependence of the microbiological action on the nature of substituents in the molecules of N-, R-alkylamines some methyl, ethylamine, aminoalcohols, N-hydroxymethyl- and N-methyl-N-carboxymethylamines have been tested. In accordance with the WHO recommendations to assess the antibacterial activity of N-, R-alkylamines the gram-positive test strains – Staphylococcus aureus ATCC 25923 and Bacillus subtilis ATCC 6633 were used. The aliphatic amines and aminoalcohols studied show a weak or moderate activity in relation to strains of Staphylococcus aureus ATCC 25923 and Bacillus subtilis ATCC 6633. Compounds containing a carboxyl group and methyl radicals in the molecule exhibit the greatest antimicrobial activity in relation to the gram-positive strains of microorganisms under research.

Highlights

Antibacterial agents are practically the only group of drugs which effectiveness decreases with time due to development of resistance
It is known that tertiary amine salts or quaternary ammonium bases containing radicals with a large number of carbon atoms exhibit a strong bacteriostatic and bactericidal action, as well as possess pronounced disinfectant properties [1, 8]
In literature there are data that compounds with the number of carbon atoms from 5 to 16 are the most effective against microorganisms [6]

Summary

Introduction

Antibacterial agents are practically the only group of drugs which effectiveness decreases with time due to development of resistance. The results of the multicentre randomized trial SCOPE (USA) published in 2004 indicate the predominance of gram-positive cocci in the etiological structure of nosocomial bacteriemias [14] This tendency creates significant problems since the choice of antimicrobial agents intended to combat drugresistant gram-positive microorganisms is limited. It should be noted the fact that antibiotics are less than 5% of the drugs being currently at the stage of drug development [5], and as resistance to the medicines used develops, there is a need in both creation of new drugs, and correction of methods for using the existing ones. The aim of this work was to determine the effect of various functional groups containing in the molecules of N-, R-alkylamines derivatives on their antibacterial activity in relation to some gram-positive strains of microorganisms

Objectives

Methods

Findings

Conclusion