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Discovery of bacterial NAD+-dependent DNA ligase inhibitors: optimization of antibacterial activity.
Bioorg Med Chem Lett
; 21(15): 4556-60, 2011 Aug 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-21719282
RESUMEN
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.