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In vitro antibacterial and antifungal activity of salicylanilide pyrazine-2-carboxylates
Martin Krátký, Jarmila Vinšová, Vladimír Buchta
Jazyk angličtina Země Nizozemsko
Typ dokumentu časopisecké články, práce podpořená grantem
Grantová podpora
NS10367
MZ0
CEP - Centrální evidence projektů
- MeSH
- antibakteriální látky chemie farmakologie MeSH
- antifungální látky chemie farmakologie MeSH
- gramnegativní bakterie účinky léků MeSH
- houby účinky léků MeSH
- mikrobiální testy citlivosti MeSH
- molekulární struktura MeSH
- pyraziny chemie farmakologie MeSH
- salicylanilidy chemie farmakologie MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
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 μmol/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 μmol/L). The most active antifungal agent overall proved to be 2-(4-bromophenylcarbamoyl)-4-chlorophenyl pyrazine-2-carboxylate.
Citace poskytuje Crossref.org
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- $a Krátký, Martin $u Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Hradec Králové, the Czech Republic
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- $a In vitro antibacterial and antifungal activity of salicylanilide pyrazine-2-carboxylates / $c Martin Krátký, Jarmila Vinšová, Vladimír Buchta
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- $a 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 μmol/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 μmol/L). The most active antifungal agent overall proved to be 2-(4-bromophenylcarbamoyl)-4-chlorophenyl pyrazine-2-carboxylate.
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- $a Buchta, Vladimír $u Department of Clinical Microbiology, Faculty of Medicine and University Hospital, Charles University, Hradec Králové, the Czech Republic; Department of Biological and Medical Sciences, Faculty of Pharmacy, Charles University, Hradec Králové, the Czech Republic
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