Literature DB >> 29773506

In vitro activity of salicylamide derivatives against vancomycin-resistant enterococci.

Sarka Pospisilova1, Hana Michnova1, Tereza Kauerova2, Karel Pauk3, Peter Kollar2, Jarmila Vinsova4, Ales Imramovsky3, Alois Cizek5, Josef Jampilek6.   

Abstract

A series of 13 salicylamide derivatives was assessed for antibacterial activity against three isolates of vancomycin-resistant Enterococcus faecalis (VRE) and Enterococcus faecalis ATCC 29212 as a quality standard. The minimum inhibitory concentration was determined by the broth microdilution method with subsequent subcultivation of aliquots to assess minimum bactericidal concentration. The growth kinetics was established by the time-kill assay. Ampicillin, ciprofloxacin, tetracycline and vancomycin were used as the reference antibacterial drugs. Three of the investigated compounds showed strong bacteriostatic activity against VRE (0.199-25 µM) comparable to or more potent than ampicillin and ciprofloxacin. In addition, these compounds were tested for synergistic effect with vancomycin, ciprofloxacin and tetracycline, while 5-chloro-2-hydroxy-N-[4-(trifluoromethyl)phenyl]benzamide showed the highest potency as well as synergistic activity with vancomycin against VRE 368. Screening of the cytotoxicity of the most effective compounds was performed using human monocytic leukemia THP-1 cells, and based on LD50 values, it can be stated that the compounds have insignificant toxicity against human cells.
Copyright © 2018 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Antibacterial activity; Cytotoxicity; Enterococcus; Salicylamides; Time-kill assay

Mesh:

Substances:

Year:  2018        PMID: 29773506     DOI: 10.1016/j.bmcl.2018.05.011

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

1.  Repurposing salicylamide for combating multidrug-resistant Neisseria gonorrhoeae.

Authors:  Marwa Alhashimi; Abdelrahman Mayhoub; Mohamed N Seleem
Journal:  Antimicrob Agents Chemother       Date:  2019-09-30       Impact factor: 5.191

2.  Design and synthesis of anticancer 1-hydroxynaphthalene-2-carboxanilides with a p53 independent mechanism of action.

Authors:  Ewelina Spaczyńska; Anna Mrozek-Wilczkiewicz; Katarzyna Malarz; Jiri Kos; Tomas Gonec; Michal Oravec; Robert Gawecki; Andrzej Bak; Jana Dohanosova; Iva Kapustikova; Tibor Liptaj; Josef Jampilek; Robert Musiol
Journal:  Sci Rep       Date:  2019-04-23       Impact factor: 4.379

3.  Synthesis and Spectrum of Biological Activities of Novel N-arylcinnamamides.

Authors:  Sarka Pospisilova; Jiri Kos; Hana Michnova; Iva Kapustikova; Tomas Strharsky; Michal Oravec; Agnes M Moricz; Jozsef Bakonyi; Tereza Kauerova; Peter Kollar; Alois Cizek; Josef Jampilek
Journal:  Int J Mol Sci       Date:  2018-08-07       Impact factor: 5.923

4.  Novel organophosphorus aminopyrimidines as unique structural DNA-targeting membrane active inhibitors towards drug-resistant methicillin-resistant Staphylococcus aureus.

Authors:  Di Li; Rammohan R Yadav Bheemanaboina; Narsaiah Battini; Vijai Kumar Reddy Tangadanchu; Xian-Fu Fang; Cheng-He Zhou
Journal:  Medchemcomm       Date:  2018-08-01       Impact factor: 3.597

  4 in total

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