Synthesis and biological activity of new salicylanilide N,N-disubstituted carbamates and thiocarbamates

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11160%2F14%3A10281766" target="_blank" >RIV/00216208:11160/14:10281766 - isvavai.cz</a>

Výsledek na webu

<a href="http://www.sciencedirect.com/science/article/pii/S0968089614004234" target="_blank" >http://www.sciencedirect.com/science/article/pii/S0968089614004234</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.bmc.2014.05.064" target="_blank" >10.1016/j.bmc.2014.05.064</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Synthesis and biological activity of new salicylanilide N,N-disubstituted carbamates and thiocarbamates

Popis výsledku v původním jazyce

The development of novel antimicrobial drugs represents a cutting edge research topic. In this study, 20 salicylanilide N,N-disubstituted carbamates and thiocarbamates were designed, synthesised and characterised by IR, H-1 NMR and C-13 NMR. The compounds were evaluated in vitro as potential antimicrobial agents against Mycobacterium tuberculosis and nontuberculous mycobacteria (Mycobacterium avium and Mycobacterium kansasii) as well as against eight bacterial and fungal strains. Additionally, we investigated the inhibitory effect of these compounds on mycobacterial isocitrate lyase and cellular toxicity. The minimum inhibitory concentrations (MICs) against mycobacteria were from 4 mu M for thiocarbamates and from 16 mu M for carbamates. Gram-positivebacteria, including methicillin-resistant Staphylococcus aureus, were inhibited with MICs from 0.49 mu M by thiocarbamates, whilst Gram-negative bacteria and most of the fungi did not display any significant susceptibility. All (thio)carb

Název v anglickém jazyce

Synthesis and biological activity of new salicylanilide N,N-disubstituted carbamates and thiocarbamates

Popis výsledku anglicky

The development of novel antimicrobial drugs represents a cutting edge research topic. In this study, 20 salicylanilide N,N-disubstituted carbamates and thiocarbamates were designed, synthesised and characterised by IR, H-1 NMR and C-13 NMR. The compounds were evaluated in vitro as potential antimicrobial agents against Mycobacterium tuberculosis and nontuberculous mycobacteria (Mycobacterium avium and Mycobacterium kansasii) as well as against eight bacterial and fungal strains. Additionally, we investigated the inhibitory effect of these compounds on mycobacterial isocitrate lyase and cellular toxicity. The minimum inhibitory concentrations (MICs) against mycobacteria were from 4 mu M for thiocarbamates and from 16 mu M for carbamates. Gram-positivebacteria, including methicillin-resistant Staphylococcus aureus, were inhibited with MICs from 0.49 mu M by thiocarbamates, whilst Gram-negative bacteria and most of the fungi did not display any significant susceptibility. All (thio)carb

Druh

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

CEP obor

FR - Farmakologie a lékárnická chemie

OECD FORD obor

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Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2014

Kód důvěrnosti údajů

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

Název periodika

Bioorganic and Medicinal Chemistry

ISSN

0968-0896

e-ISSN

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Svazek periodika

22

Číslo periodika v rámci svazku

15

Stát vydavatele periodika

GB - Spojené království Velké Británie a Severního Irska

Počet stran výsledku

10

Strana od-do

4073-4082

Kód UT WoS článku

000339859700032

EID výsledku v databázi Scopus

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