Open AccessAntibacterial activity of synthetic 1,3‐bis(aryloxy)propan‐2‐amines against Gram‐positive bacteria
Author(s) -
Serafim Mateus S. M.,
Lavorato Stefânia N.,
Kronenberger Thales,
Sousa Yamara V.,
Oliveira Graziele P.,
dos Santos Simone G.,
Kroon Erna G.,
Maltarollo Vinícius G.,
Alves Ricardo J.,
Mota Bruno E. F.
Publication year - 2019
Publication title -
microbiologyopen
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.881
H-Index - 36
ISSN - 2045-8827
DOI - 10.1002/mbo3.814
Subject(s) - enterococcus faecalis , antibacterial activity , bacteria , staphylococcus aureus , microbiology and biotechnology , chemistry , norfloxacin , ftsz , antimicrobial , streptococcus pyogenes , antiprotozoal , biology , biochemistry , antibiotics , in vitro , bacterial protein , ciprofloxacin , genetics
Synthetic 1,3‐bis(aryloxy)propan‐2‐amines have been shown in previous studies to possess several biological activities, such as antifungal and antiprotozoal. In the present study, we describe the antibacterial activity of new synthetic 1,3‐bis(aryloxy)propan‐2‐amines against Gram‐positive pathogens ( Streptococcus pyogenes , Enterococcus faecalis and Staphylococcus aureus ) including Methicillin–resistant S. aureus strains. Our compounds showed minimal inhibitory concentrations (MIC) in the range of 2.5–10 μg/ml (5.99–28.58 μM), against different bacterial strains. The minimal bactericidal concentrations found were similar to MIC, suggesting a bactericidal mechanism of action of these compounds. Furthermore, possible molecular targets were suggested by chemical similarity search followed by docking approaches. Our compounds are similar to known ligands targeting the cell division protein FtsZ , Quinolone resistance protein norA and the Enoyl‐[acyl‐carrier‐protein] reductase FabI . Taken together, our data show that synthetic 1,3‐bis(aryloxy)propan‐2‐amines are active against Gram‐positive bacteria, including multidrug–resistant strains and can be a promising lead in the development of new antibacterial compounds for the treatment of these infections.