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

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

Author information

1
Institute for Pharmaceutical Biology, University of Bonn , Bonn, Germany.
2
Interfaculty Institute of Biochemistry, University of Tübingen , Tübingen, Germany.
3
Institute for Medical Microbiology, Immunology and Parasitology, University Hospital Bonn , Bonn, Germany.
4
Leibniz Institute for Natural Product Research and Infection Biology e.V., Hans Knöll Institute , Jena, Germany.
5
Department of Biochemistry and Molecular Biology, Schools of Medicine and Dentistry, University of Alabama at Birmingham , Birmingham, Alabama, United States.

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.

PMID:
26431157
DOI:
10.1021/acs.jnatprod.5b00175
[Indexed for MEDLINE]

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