Design, synthesis and biological evaluation of potent NAD+-dependent DNA ligase inhibitors as potential antibacterial agents. Part 2: 4-Amino-pyrido[2,3-d]pyrimidin-5(8H)-ones

A series of 4-amino-pyrido[2,3-d]pyrimidin-5(8H)-ones were designed and synthesized as a novel class of inhibitors of NAD+-dependent DNA ligase that possess potency against Gram-positive bacteria.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2012-06, Vol.22 (11), p.3699-3703
Hauptverfasser:	Wang, Tiansheng, Duncan, Leonard, Gu, Wenxin, O’Dowd, Hardwin, Wei, Yunyi, Perola, Emanuele, Parsons, Jonathan, Gross, Christian H., Moody, Cameron Stuver, Ryan Arends, S.J., Charifson, Paul S.
Format:	Artikel
Sprache:	eng
Schlagworte:	Anti-Bacterial Agents - chemical synthesis Anti-Bacterial Agents - chemistry Anti-Bacterial Agents - pharmacology Antibacterial agents Antibiotics Bacterial Proteins - antagonists & inhibitors Bacterial Proteins - metabolism Binding Sites Catalytic Domain chemistry Computer Simulation Crystallography, X-Ray DNA DNA ligase DNA Ligase ATP DNA Ligases - antagonists & inhibitors DNA Ligases - metabolism Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Gram-Negative Bacteria - drug effects Gram-positive bacteria Gram-Positive Bacteria - drug effects Inhibitor Microbial Sensitivity Tests NAD NAD - metabolism Pyridopyrimidinone Pyrimidinones - chemistry Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	A series of 4-amino-pyrido[2,3-d]pyrimidin-5(8H)-ones were designed and synthesized as a novel class of inhibitors of NAD+-dependent DNA ligase that possess potency against Gram-positive bacteria.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2012.04.038