Combating highly resistant emerging pathogen Mycobacterium abscessus and Mycobacterium tuberculosis with novel salicylanilide esters and carbamates

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11160%2F15%3A10312612" target="_blank" >RIV/00216208:11160/15:10312612 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/71009396:_____/15:N0000008

Výsledek na webu

<a href="http://www.sciencedirect.com/science/article/pii/S0223523415301331" target="_blank" >http://www.sciencedirect.com/science/article/pii/S0223523415301331</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.ejmech.2015.07.001" target="_blank" >10.1016/j.ejmech.2015.07.001</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Combating highly resistant emerging pathogen Mycobacterium abscessus and Mycobacterium tuberculosis with novel salicylanilide esters and carbamates

Popis výsledku v původním jazyce

Based on previous results, a series of salicylanilides, salicylanilide 5-chloropyrazinoates and carbamates was designed, synthesized and characterised. The compounds were evaluated for their in vitro activity on M. abscessus, susceptible M. tuberculosisH(37)Rv, multidrug-resistant (MDR) M. tuberculosis MDR A8, M. tuberculosis MDR 9449/2006 and on the extremely-resistant Praha 131 (XDR) strains. All derivatives exhibited a significant activity with minimum inhibitory concentrations (MICs) in the low micromolar range. Eight salicylanilide carbamates and two salicylanilide esters exhibited an excellent in vitro activity on M. abscessus with MICs from 0.2 to 2.1 mu M, thus being more effective than ciprofloxacin and gentamicin. This finding is potentiallypromising, particularly, as M. abscessus is a threateningly chemotherapy-resistant species. M. tuberculosis H(37)Rv was inhibited with MICs from 0.2 mu M, and eleven compounds have lower MICs than isoniazid. Salicylanilide esters and car

Název v anglickém jazyce

Combating highly resistant emerging pathogen Mycobacterium abscessus and Mycobacterium tuberculosis with novel salicylanilide esters and carbamates

Popis výsledku anglicky

Based on previous results, a series of salicylanilides, salicylanilide 5-chloropyrazinoates and carbamates was designed, synthesized and characterised. The compounds were evaluated for their in vitro activity on M. abscessus, susceptible M. tuberculosisH(37)Rv, multidrug-resistant (MDR) M. tuberculosis MDR A8, M. tuberculosis MDR 9449/2006 and on the extremely-resistant Praha 131 (XDR) strains. All derivatives exhibited a significant activity with minimum inhibitory concentrations (MICs) in the low micromolar range. Eight salicylanilide carbamates and two salicylanilide esters exhibited an excellent in vitro activity on M. abscessus with MICs from 0.2 to 2.1 mu M, thus being more effective than ciprofloxacin and gentamicin. This finding is potentiallypromising, particularly, as M. abscessus is a threateningly chemotherapy-resistant species. M. tuberculosis H(37)Rv was inhibited with MICs from 0.2 mu M, and eleven compounds have lower MICs than isoniazid. Salicylanilide esters and car

Druh

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

CEP obor

FR - Farmakologie a lékárnická chemie

OECD FORD obor

—

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

2015

Kód důvěrnosti údajů

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

Název periodika

European Journal of Medicinal Chemistry

ISSN

0223-5234

e-ISSN

—

Svazek periodika

101

Číslo periodika v rámci svazku

August

Stát vydavatele periodika

FR - Francouzská republika

Počet stran výsledku

13

Strana od-do

692-704

Kód UT WoS článku

000360771900059

EID výsledku v databázi Scopus

2-s2.0-84937925828