Discovery and structure-activity relationships of a novel isothiazolone class of bacterial type II topoisomerase inhibitors.
Bioorg Med Chem Lett
; 26(17): 4179-83, 2016 09 01.
Article
em En
| MEDLINE
| ID: mdl-27499455
ABSTRACT
There is an urgent and unmet medical need for new antibacterial drugs that tackle infections caused by multidrug-resistant (MDR) pathogens. During the course of our wider efforts to discover and exploit novel mechanism of action antibacterials, we have identified a novel series of isothiazolone based inhibitors of bacterial type II topoisomerase. Compounds from the class displayed excellent activity against both Gram-positive and Gram-negative bacteria with encouraging activity against a panel of MDR clinical Escherichia coli isolates when compared to ciprofloxacin. Representative compounds also displayed a promising in vitro safety profile.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Tiazóis
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DNA Topoisomerases Tipo II
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Tiazolidinas
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Inibidores da Topoisomerase II
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Antibacterianos
Limite:
Humans
Idioma:
En
Ano de publicação:
2016
Tipo de documento:
Article