Discovery of bacterial NAD+-dependent DNA ligase inhibitors: optimization of antibacterial activity.
Bioorg Med Chem Lett
; 21(15): 4556-60, 2011 Aug 01.
Article
em En
| MEDLINE
| ID: mdl-21719282
ABSTRACT
Optimization of adenosine analog inhibitors of bacterial NAD(+)-dependent DNA ligase is discussed. Antibacterial activity against Streptococcus pneumoniae and Staphylococcus aureus was improved by modification of the 2-position substituent on the adenine ring and 3'- and 5'-substituents on the ribose. Compounds with logD values 1.5-2.5 maximized potency and maintained drug-like physical properties.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
DNA Ligases
/
Inibidores Enzimáticos
/
Antibacterianos
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article