Novel hydroxyl tricyclics (e.g., GSK966587) as potent inhibitors of bacterial type IIA topoisomerases.
Bioorg Med Chem Lett
; 23(19): 5437-41, 2013 Oct 01.
Article
em En
| MEDLINE
| ID: mdl-23968823
ABSTRACT
During the course of our research to find novel mode of action antibacterials, we discovered a series of hydroxyl tricyclic compounds that showed good potency against Gram-positive and Gram-negative pathogens. These compounds inhibit bacterial type IIA topoisomerases. Herein we will discuss structure-activity relationships in this series and report advanced studies on compound 1 (GSK966587) which demonstrates good PK and in vivo efficacy properties. X-ray crystallographic studies were used to provide insight into the structural basis for the difference in antibacterial potency between enantiomers.
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Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Bactérias
/
Inibidores da Topoisomerase II
/
Naftiridinas
Idioma:
En
Ano de publicação:
2013
Tipo de documento:
Article
País de afiliação:
Espanha