Literature DB >> 26431157

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

Till F Schäberle1, Alexander Schmitz1, Georg Zocher2, Andrea Schiefer3, Stefan Kehraus1, Edith Neu1, Martin Roth4, Dmitry G Vassylyev5, Thilo Stehle2, Gabriele Bierbaum3, Achim Hoerauf3, Kenneth Pfarr3, Gabriele M König1.   

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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Year:  2015        PMID： 26431157     DOI： 10.1021/acs.jnatprod.5b00175

Source DB:  PubMed          Journal:  J Nat Prod        ISSN： 0163-3864            Impact factor:   4.050


  12 in total

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2.  Orientia tsutsugamushi Is Highly Susceptible to the RNA Polymerase Switch Region Inhibitor Corallopyronin A In Vitro and In Vivo.

Authors:  Fredericke Kock; Matthias Hauptmann; Anke Osterloh; Till F Schäberle; Sven Poppert; Hagen Frickmann; Klaus-Dieter Menzel; Gundela Peschel; Kenneth Pfarr; Andrea Schiefer; Gabriele M König; Achim Hoerauf; Bernhard Fleischer; Christian Keller
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