Insights into Structure-Activity Relationships of Bacterial RNA Polymerase Inhibiting Corallopyronin Derivatives
| Autor: | Martin Roth, Achim Hoerauf, Alexander Schmitz, Kenneth Pfarr, Dmitry G. Vassylyev, Gabriele Bierbaum, Till F. Schäberle, Gabriele M. König, Thilo Stehle, Andrea Schiefer, Edith Neu, Georg Zocher, Stefan Kehraus |
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| Rok vydání: | 2015 |
| Předmět: |
medicine.drug_class
Stereochemistry Antibiotics Pharmaceutical Science Biology Analytical Chemistry chemistry.chemical_compound Lactones Structure-Activity Relationship Biosynthesis Belgium Drug Discovery medicine Structure–activity relationship Myxococcales Derivatization Polymerase Soil Microbiology Pharmacology Natural product Strain (chemistry) Organic Chemistry DNA-Directed RNA Polymerases Into-structure Anti-Bacterial Agents Complementary and alternative medicine chemistry Biochemistry biology.protein Molecular Medicine |
| Zdroj: | Journal of natural products. 78(10) |
| ISSN: | 1520-6025 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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