In Vitro Antibacterial and Antifungal Activity of Salicylanilide Pyrazine-2-carboxylates

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00179906%3A_____%2F12%3A10128912" target="_blank" >RIV/00179906:_____/12:10128912 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/00216208:11150/12:10128912 RIV/00216208:11160/12:10128912

Výsledek na webu

<a href="http://www.ingentaconnect.com/content/ben/mc/2012/00000008/00000004/art00028" target="_blank" >http://www.ingentaconnect.com/content/ben/mc/2012/00000008/00000004/art00028</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.2174/157340612801216346" target="_blank" >10.2174/157340612801216346</a>

Jazyk výsledku

angličtina

Název v původním jazyce

In Vitro Antibacterial and Antifungal Activity of Salicylanilide Pyrazine-2-carboxylates

Popis výsledku v původním jazyce

The development of new antimicrobial agents for the treatment of infectious diseases remains challenging due to the increasing impact of antibiotic resistance. Since salicylanilides and esters of pyrazine-2-carboxylic acid have been described as potential antimicrobials, we have designed and synthesized a series of 2-(phenylcarbamoyl) phenyl pyrazine-2-carboxylates. These were evaluated in vitro for the activity against fungi and Gram-positive and Gram-negative bacteria. All derivatives showed significant antibacterial activity against Gram-positive strains (MIC }= 0.98 mu mol/L) including methicillin-resistant Staphylococcus aureus. The most active molecule was 5-chloro-2-(3-chlorophenylcarbamoyl) phenyl pyrazine-2-carboxylate. With one exception these esters were at least partly active against fungi tested strains, in particular against mould strains (MIC }= 1.95 mu mol/L). The most active antifungal agent overall proved to be 2-(4-bromophenylcarbamoyl)-4-chlorophenyl pyrazine-2-carboxylate.

Název v anglickém jazyce

In Vitro Antibacterial and Antifungal Activity of Salicylanilide Pyrazine-2-carboxylates

Popis výsledku anglicky

The development of new antimicrobial agents for the treatment of infectious diseases remains challenging due to the increasing impact of antibiotic resistance. Since salicylanilides and esters of pyrazine-2-carboxylic acid have been described as potential antimicrobials, we have designed and synthesized a series of 2-(phenylcarbamoyl) phenyl pyrazine-2-carboxylates. These were evaluated in vitro for the activity against fungi and Gram-positive and Gram-negative bacteria. All derivatives showed significant antibacterial activity against Gram-positive strains (MIC }= 0.98 mu mol/L) including methicillin-resistant Staphylococcus aureus. The most active molecule was 5-chloro-2-(3-chlorophenylcarbamoyl) phenyl pyrazine-2-carboxylate. With one exception these esters were at least partly active against fungi tested strains, in particular against mould strains (MIC }= 1.95 mu mol/L). The most active antifungal agent overall proved to be 2-(4-bromophenylcarbamoyl)-4-chlorophenyl pyrazine-2-carboxylate.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

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OECD FORD obor

10606 - Microbiology

Projekt

<a href="/cs/project/NS10367" target="_blank" >NS10367: Hodnocení a vývoj nových perspektivních antituberkulotik a jejich proléčiv aktivních vůči multirezistentním kmenům</a><br>

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

2012

Kód důvěrnosti údajů

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

Název periodika

Medicinal Chemistry

ISSN

1573-4064

e-ISSN

—

Svazek periodika

8

Číslo periodika v rámci svazku

4

Stát vydavatele periodika

NL - Nizozemsko

Počet stran výsledku

10

Strana od-do

732-741

Kód UT WoS článku

000309524600028

EID výsledku v databázi Scopus

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