Insights into Structure-Activity Relationships of Bacterial RNA Polymerase Inhibiting Corallopyronin Derivatives

J Nat Prod. 2015 Oct 23;78(10):2505-9. doi: 10.1021/acs.jnatprod.5b00175. Epub 2015 Oct 2.

Abstract

The new compound precorallopyronin A is a stable precursor in the biosynthesis of the antibiotic corallopyronin A. This natural product was isolated from the producer strain Corallococcus coralloides B035. Together with various semisynthetically obtained corallopyronin A derivatives its antibacterial effects were evaluated. In combination with an X-ray crystallization model limitations of derivatization possibilities were revealed. The antibiotic potential of the novel precorallopyronin A is comparable to that of the structurally more complex corallopyronin A, which highlights that the additional chiral center is not essential for activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology
  • Belgium
  • DNA-Directed RNA Polymerases / antagonists & inhibitors*
  • Lactones / chemistry*
  • Lactones / isolation & purification
  • Lactones / pharmacology
  • Myxococcales / chemistry*
  • Soil Microbiology
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Lactones
  • corallopyronin A
  • DNA-Directed RNA Polymerases