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

Ricardo Lira; Alan X Xiang; Thomas Doundoulakis; William T Biller; Konstantinos A Agrios; Klaus B Simonsen; Stephen E Webber; Wes Sisson; Robert M Aust; Amit M Shah; Richard E Showalter; Virginia N Banh; Kevin R Steffy; James R Appleman

doi:10.1016/j.bmcl.2007.10.017

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

Bioorg Med Chem Lett. 2007 Dec 15;17(24):6797-800. doi: 10.1016/j.bmcl.2007.10.017. Epub 2007 Oct 17.

Authors

Ricardo Lira¹, Alan X Xiang, Thomas Doundoulakis, William T Biller, Konstantinos A Agrios, Klaus B Simonsen, Stephen E Webber, Wes Sisson, Robert M Aust, Amit M Shah, Richard E Showalter, Virginia N Banh, Kevin R Steffy, James R Appleman

Affiliation

¹ Anadys Pharmaceuticals, Inc., 3115 Merryfield Row, San Diego, CA 92121, USA.

PMID: 17980587
DOI: 10.1016/j.bmcl.2007.10.017

Abstract

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.

MeSH terms

Anti-Bacterial Agents / chemical synthesis
Anti-Bacterial Agents / chemistry
Anti-Bacterial Agents / pharmacology
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*
Methylation
Molecular Structure
Staphylococcus aureus / drug effects
Staphylococcus aureus / enzymology

Substances

Anti-Bacterial Agents
Enzyme Inhibitors
Lactones
myxopyronin B
DNA-Directed RNA Polymerases