title: Insights into Structure-Activity Relationships of Bacterial RNA Polymerase Inhibiting Corallopyronin Derivatives.
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.
authors.affiliation: Institute for Pharmaceutical Biology, University of Bonn , Bonn, Germany.
authors.forename: Till F
authors.initials: TF
authors.lastname: Schäberle
authors.affiliation: Institute for Pharmaceutical Biology, University of Bonn , Bonn, Germany.
authors.forename: Alexander
authors.initials: A
authors.lastname: Schmitz
authors.affiliation: Interfaculty Institute of Biochemistry, University of Tübingen , Tübingen, Germany.
authors.forename: Georg
authors.initials: G
authors.lastname: Zocher
authors.affiliation: Institute for Medical Microbiology, Immunology and Parasitology, University Hospital Bonn , Bonn, Germany.
authors.forename: Andrea
authors.initials: A
authors.lastname: Schiefer
authors.affiliation: Institute for Pharmaceutical Biology, University of Bonn , Bonn, Germany.
authors.forename: Stefan
authors.initials: S
authors.lastname: Kehraus
authors.affiliation: Institute for Pharmaceutical Biology, University of Bonn , Bonn, Germany.
authors.forename: Edith
authors.initials: E
authors.lastname: Neu
authors.affiliation: Leibniz Institute for Natural Product Research and Infection Biology e.V., Hans Knöll Institute , Jena, Germany.
authors.forename: Martin
authors.initials: M
authors.lastname: Roth
authors.affiliation: Department of Biochemistry and Molecular Biology, Schools of Medicine and Dentistry, University of Alabama at Birmingham , Birmingham, Alabama, United States.
authors.forename: Dmitry G
authors.initials: DG
authors.lastname: Vassylyev
authors.affiliation: Interfaculty Institute of Biochemistry, University of Tübingen , Tübingen, Germany.
authors.forename: Thilo
authors.initials: T
authors.lastname: Stehle
authors.affiliation: Institute for Medical Microbiology, Immunology and Parasitology, University Hospital Bonn , Bonn, Germany.
authors.forename: Gabriele
authors.initials: G
authors.lastname: Bierbaum
authors.affiliation: Institute for Medical Microbiology, Immunology and Parasitology, University Hospital Bonn , Bonn, Germany.
authors.forename: Achim
authors.initials: A
authors.lastname: Hoerauf
authors.affiliation: Institute for Medical Microbiology, Immunology and Parasitology, University Hospital Bonn , Bonn, Germany.
authors.forename: Kenneth
authors.initials: K
authors.lastname: Pfarr
authors.affiliation: Institute for Pharmaceutical Biology, University of Bonn , Bonn, Germany.
authors.forename: Gabriele M
authors.initials: GM
authors.lastname: König
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology; D001530:Belgium; D012321:DNA-Directed RNA Polymerases / Q000037:antagonists & inhibitors*; D007783:Lactones / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D009231:Myxococcales / Q000737:chemistry*; D012988:Soil Microbiology; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D007783:Lactones; C532894:corallopyronin A; D012321:DNA-Directed RNA Polymerases