Abstract
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.
Keywords: Antibacterial activity, antifungal activity, in vitro activity, pyrazine-2-carboxylic acid ester, salicylanilide, salicylanilide ester, salicylanilide, Clostridium difficile, Staphylococcus aureus, MRSA, fungal pathogens
Medicinal Chemistry
Title:In Vitro Antibacterial and Antifungal Activity of Salicylanilide Pyrazine-2- carboxylates
Volume: 8 Issue: 4
Author(s): Martin Kratky, Jarmila Vinsova and Vladimir Buchta
Affiliation:
Keywords: Antibacterial activity, antifungal activity, in vitro activity, pyrazine-2-carboxylic acid ester, salicylanilide, salicylanilide ester, salicylanilide, Clostridium difficile, Staphylococcus aureus, MRSA, fungal pathogens
Abstract: 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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Cite this article as:
Kratky Martin, Vinsova Jarmila and Buchta Vladimir, In Vitro Antibacterial and Antifungal Activity of Salicylanilide Pyrazine-2- carboxylates, Medicinal Chemistry 2012; 8 (4) . https://dx.doi.org/10.2174/157340612801216346
DOI https://dx.doi.org/10.2174/157340612801216346 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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