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

Schäberle TF, Schmitz A, Zocher G, Schiefer A, Kehraus S, Neu E, Roth M, Vassylyev DG, Stehle T, Bierbaum G, Hoerauf A, Pfarr K, König GM (2015) Insights into Structure–Activity Relationships of Bacterial RNA Polymerase Inhibiting Corallopyronin Derivatives J Nat Prod 78(10), 2505-2509. PubMed Supplement

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.

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doi: 10.1021 PMID: 26431157