Negishi cross-coupling enabled synthesis of novel NAD+-dependent DNA ligase inhibitors and SAR development

[Display omitted] Two novel compounds, pyridopyrimidines (1) and naphthyridines (2) were identified as potent inhibitors of bacterial NAD+-dependent DNA ligase (Lig) A in a fragment screening. SAR was guided by molecular modeling and X-ray crystallography. It was observed that the diaminonitrile pha...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2015-11, Vol.25 (22), p.5172-5177
Hauptverfasser:	Murphy-Benenato, Kerry E., Gingipalli, Lakshmaiah, Boriack-Sjodin, P. Ann, Martinez-Botella, Gabriel, Carcanague, Dan, Eyermann, Charles J., Gowravaram, Madhu, Harang, Jenna, Hale, Michael R., Ioannidis, Georgine, Jahic, Harris, Johnstone, Michele, Kutschke, Amy, Laganas, Valerie A., Loch, James T., Miller, Matthew D., Oguto, Herbert, Patel, Sahil Joe
Format:	Artikel
Sprache:	eng
Schlagworte:	Anti-Bacterial Agents - chemical synthesis Anti-Bacterial Agents - pharmacology Antibacterial Bacterial Proteins - antagonists & inhibitors Bacterial Proteins - chemistry Cross-coupling Diaminonitrile DNA Ligases - antagonists & inhibitors DNA Ligases - chemistry Haemophilus influenzae - drug effects Microbial Sensitivity Tests NAD - metabolism NAD+-dependent ligase resistance Naphthyridines - chemical synthesis Naphthyridines - pharmacology Pyridopyrimidine Pyrimidines - chemical synthesis Pyrimidines - pharmacology Staphylococcus aureus - drug effects Streptococcus pneumoniae - drug effects Structure-Activity Relationship
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