Syntheses of novel myxopyronin B analogs as potential inhibitors of bacterial RNA polymerase

• Published in: Bioorganic & medicinal chemistry letters Vol. 17; no. 24; pp. 6797 - 6800
• Main Authors: Lira, Ricardo, Xiang, Alan X., Doundoulakis, Thomas, Biller, William T., Agrios, Konstantinos A., Simonsen, Klaus B., Webber, Stephen E., Sisson, Wes, Aust, Robert M., Shah, Amit M., Showalter, Richard E., Banh, Virginia N., Steffy, Kevin R., Appleman, James R.
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 15.12.2007; Elsevier
• Subjects: Anti-Bacterial Agents - chemical synthesis; Anti-Bacterial Agents - chemistry; Anti-Bacterial Agents - pharmacology; Antibacterial; Antibacterial agents; Antibiotics; Antibiotics. Antiinfectious agents. Antiparasitic agents; Biological and medical sciences; Curtius rearrangement; DNA-Directed RNA Polymerases - antagonists & inhibitors; DNA-Directed RNA Polymerases - metabolism; Enzyme Inhibitors - chemical synthesis; Enzyme Inhibitors - chemistry; Enzyme Inhibitors - pharmacology; Escherichia coli - drug effects; Escherichia coli - enzymology; Inhibitory Concentration 50; Lactones - chemical synthesis; Lactones - chemistry; Lactones - pharmacology; Medical sciences; Methylation; Molecular Structure; Myxopyronin B; Ortholithiation; Pharmacology. Drug treatments; Staphylococcus aureus - drug effects; Staphylococcus aureus - enzymology; Ortholithiation; Curtius rearrangement; Antibacterial; Antibiotics; Myxopyronin B; Enzyme; Transferases; Escherichia coli; Enzyme inhibitor; Lactone; Organic carbamate; DNA-directed RNA polymerase; In vitro; Nucleotidyltransferases; Antibiotic; Lithiation; Structure activity relation; Bacteria; Micrococcales; Micrococcaceae; Antibacterial agent; Chemical synthesis; Staphylococcus aureus; Enterobacteriaceae
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2007.10.017

Novel myxopyronin B analogs have been prepared and tested for in vitro inhibitory activity against DNA-dependent RNA polymerase and antibacterial activity against Escherichia coli and Staphylococcus aureus. Based upon observations from our initial findings, additional myxopyronin B analogs have been prepared and tested for in vitro inhibitory activity against DNA-dependent RNA polymerase and antibacterial activity against Escherichia coli and Staphylococcus aureus.