Synthesis and antimicrobial activity of sulphamethoxazole-based ureas and imidazolidine-2,4,5-triones

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11150%2F15%3A10312631" target="_blank" >RIV/00216208:11150/15:10312631 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/00216208:11160/15:10312631 RIV/00179906:_____/15:10312631

Výsledek na webu

<a href="http://www.degruyter.com/view/j/chempap.2015.69.issue-8/chempap-2015-0109/chempap-2015-0109.xml" target="_blank" >http://www.degruyter.com/view/j/chempap.2015.69.issue-8/chempap-2015-0109/chempap-2015-0109.xml</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1515/chempap-2015-0109" target="_blank" >10.1515/chempap-2015-0109</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Synthesis and antimicrobial activity of sulphamethoxazole-based ureas and imidazolidine-2,4,5-triones

Popis výsledku v původním jazyce

Progression of drug resistance among bacterial and fungal pathogens justifies the development of novel antimicrobial agents. Thus, a series of novel sulphamethoxazole-based ureas and imidazolidine-2,4,5-triones have been designed and synthesised. The urea derivatives were obtained by the reaction of sulphamethoxazole and isocyanates, and their cyclisation to imidazolidine-2,4,5-triones was performed via oxalyl chloride. All synthesised derivatives were evaluated in vitro to determine their activity against gram-positive and gram-negative bacteria, fungi, Mycobacterium tuberculosis, and atypical mycobacteria and their cytotoxicity. The growth of mycobacteria was inhibited within the range of 4-1000 mu M and M. tuberculosis was the least-susceptible strain. 4-(3-Heptylureido)-N-(5-methylisoxazol-3-yl)benzenesulphonamide was identified as the most promising compound because it exhibited the highest activity against atypical mycobacteria at minimum inhibitory concentrations, from 4 mu M, a

Název v anglickém jazyce

Synthesis and antimicrobial activity of sulphamethoxazole-based ureas and imidazolidine-2,4,5-triones

Popis výsledku anglicky

Progression of drug resistance among bacterial and fungal pathogens justifies the development of novel antimicrobial agents. Thus, a series of novel sulphamethoxazole-based ureas and imidazolidine-2,4,5-triones have been designed and synthesised. The urea derivatives were obtained by the reaction of sulphamethoxazole and isocyanates, and their cyclisation to imidazolidine-2,4,5-triones was performed via oxalyl chloride. All synthesised derivatives were evaluated in vitro to determine their activity against gram-positive and gram-negative bacteria, fungi, Mycobacterium tuberculosis, and atypical mycobacteria and their cytotoxicity. The growth of mycobacteria was inhibited within the range of 4-1000 mu M and M. tuberculosis was the least-susceptible strain. 4-(3-Heptylureido)-N-(5-methylisoxazol-3-yl)benzenesulphonamide was identified as the most promising compound because it exhibited the highest activity against atypical mycobacteria at minimum inhibitory concentrations, from 4 mu M, a

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)

Rok uplatnění

2015

Kód důvěrnosti údajů

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

Název periodika

Chemical Papers

ISSN

0366-6352

e-ISSN

—

Svazek periodika

69

Číslo periodika v rámci svazku

8

Stát vydavatele periodika

SK - Slovenská republika

Počet stran výsledku

10

Strana od-do

1108-1117

Kód UT WoS článku

000354752200012

EID výsledku v databázi Scopus

2-s2.0-84934883047