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Salicylanilide carbamates: Promising antibacterial agents with high in vitro activity against methicillin-resistant Staphylococcus aureus (MRSA)

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216275%3A25310%2F15%3A39900618" target="_blank" >RIV/00216275:25310/15:39900618 - isvavai.cz</a>

  • Alternative codes found

    RIV/00216208:11160/15:10312611 RIV/62157124:16170/15:43873571 RIV/62157124:16370/15:43873571 RIV/62157124:16810/15:43873571

  • Result on the web

    <a href="http://dx.doi.org/10.1016/j.ejps.2015.06.009" target="_blank" >http://dx.doi.org/10.1016/j.ejps.2015.06.009</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.1016/j.ejps.2015.06.009" target="_blank" >10.1016/j.ejps.2015.06.009</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

    Salicylanilide carbamates: Promising antibacterial agents with high in vitro activity against methicillin-resistant Staphylococcus aureus (MRSA)

  • Original language description

    A series of twenty-one salicylanilide N-alkylcarbamates was assessed for novel antibacterial characteristics against three clinical isolates of methicillin-resistant Staphylococcus aureus (MRSA) and S. aureus ATCC 29213 as the reference and quality control strain. The minimum inhibitory concentration was determined by the broth dilution micro-method with subsequent subcultivation of aliquots to assess minimum bactericidal concentration. The bactericidal kinetics was established by time-kill assay. Ampicillin, ciprofloxacin and vancomycin were used as reference antibacterial drugs. All the tested compounds exhibited highly potent anti-MRSA activity ({= 0.008-4 mu g/mL) comparable or up to 250x higher than that of vancomycin, the standard in the treatment of serious MRSA infections. 4-Chloro-2-(3,4-di chlorophenylcarbamoyl)phenyl butylcarbamate and 4-chloro-2-(3,4-dichlorophenylcarbamoyl)phenyl ethylcarbamate were the most active compounds. In most cases, compounds provided reliable bacteriostatic activity, except for 4-chloro-2-(4-chlorophenylcarbamoyl)phenyl decylcarbamate exhibiting bactericidal effect at 8 h (for clinical isolate of MRSA 63718) and at 24 h (for clinical isolates of MRSA SA 630 and MRSA SA 3202) at 4x MIC. Structure-activity relationships are discussed.

  • Czech name

  • Czech description

Classification

  • Type

    J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

  • CEP classification

    FR - Pharmacology and apothecary chemistry

  • OECD FORD branch

Result continuities

  • Project

    <a href="/en/project/ED1.1.00%2F02.0068" target="_blank" >ED1.1.00/02.0068: Central european institute of technology</a><br>

  • Continuities

    I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Others

  • Publication year

    2015

  • Confidentiality

    S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Data specific for result type

  • Name of the periodical

    European Journal of Pharmaceutical Sciences

  • ISSN

    0928-0987

  • e-ISSN

  • Volume of the periodical

    77

  • Issue of the periodical within the volume

    September 2015

  • Country of publishing house

    NL - THE KINGDOM OF THE NETHERLANDS

  • Number of pages

    11

  • Pages from-to

    197-207

  • UT code for WoS article

    000358975600022

  • EID of the result in the Scopus database