Pyrrolamide DNA gyrase inhibitors: optimization of antibacterial activity and efficacy.
Bioorg Med Chem Lett
; 21(24): 7416-20, 2011 Dec 15.
Article
em En
| MEDLINE
| ID: mdl-22041057
ABSTRACT
The pyrrolamides are a new class of antibacterial agents targeting DNA gyrase, an essential enzyme across bacterial species and inhibition results in the disruption of DNA synthesis and subsequently, cell death. The optimization of biochemical activity and other drug-like properties through substitutions to the pyrrole, piperidine, and heterocycle portions of the molecule resulted in pyrrolamides with improved cellular activity and in vivo efficacy.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Pirróis
/
Inibidores Enzimáticos
/
Inibidores da Topoisomerase II
/
Amidas
/
Antibacterianos
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article