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
en 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.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Tiazoles
/
ADN-Topoisomerasas de Tipo II
/
Tiazolidinas
/
Inhibidores de Topoisomerasa II
/
Antibacterianos
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2016
Tipo del documento:
Article