Antibacterial activity of a series of N2,N4-disubstituted quinazoline-2,4-diamines.
J Med Chem
; 57(7): 3075-93, 2014 Apr 10.
Article
em En
| MEDLINE
| ID: mdl-24625106
ABSTRACT
A series of N(2),N(4)-disubstituted quinazoline-2,4-diamines has been synthesized and tested against multidrug resistant Staphylococcus aureus. A structure-activity and structure-property relationship study was conducted to identify new hit compounds. This study led to the identification of N(2),N(4)-disubstituted quinazoline-2,4-diamines with minimum inhibitory concentrations (MICs) in the low micromolar range in addition to favorable physicochemical properties. Testing of biological activity revealed limited potential for resistance to these agents, low toxicity, and highly effective in vivo activity, even with low dosing regimens. Collectively, these characteristics make this compound series a suitable platform for future development of antibacterial agents.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Peritonite
/
Quinazolinas
/
Staphylococcus aureus
/
Diaminas
/
Antibacterianos
Tipo de estudo:
Prognostic_studies
Limite:
Animals
/
Humans
Idioma:
En
Revista:
J Med Chem
Assunto da revista:
QUIMICA
Ano de publicação:
2014
Tipo de documento:
Article
País de afiliação:
Estados Unidos