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

Kód výsledku v 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>

Nalezeny alternativní kódy

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

Výsledek na webu

<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>

Jazyk výsledku

angličtina

Název v původním jazyce

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

Popis výsledku v původním jazyce

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.

Název v anglickém jazyce

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

Popis výsledku anglicky

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.

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

FR - Farmakologie a lékárnická chemie

OECD FORD obor

—

Projekt

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

Návaznosti

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2015

Kód důvěrnosti údajů

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

Název periodika

European Journal of Pharmaceutical Sciences

ISSN

0928-0987

e-ISSN

—

Svazek periodika

77

Číslo periodika v rámci svazku

September 2015

Stát vydavatele periodika

NL - Nizozemsko

Počet stran výsledku

11

Strana od-do

197-207

Kód UT WoS článku

000358975600022

EID výsledku v databázi Scopus

—