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Highly Selective Electrosynthesis of 1-1-Hydroxyquinol-4-ones-Synthetic Access to Versatile Natural Antibiotics.
Org Process Res Dev
October 2024
Department of Chemistry, Johannes Gutenberg University, Duesbergweg 10-14, 55128 Mainz, Germany.
Article Synopsis
- 1-1-Hydroxyquinolin-4-ones are important biologically active compounds with a specific nitrogen-oxygen structure.
- A new electrosynthesis method allows for the efficient and eco-friendly creation of these compounds through nitro reduction, beginning with common 2-nitrobenzoic acids.
- The effectiveness of this method was proven with 26 different examples, achieving yields up to 93%, and it has significant practical applications, including the production of antibiotics like Aurachin C and HQNO.
Exploring the Diversity and Specificity of Secondary Biosynthetic Potential in .
Mar Drugs
September 2024
College of Pharmaceutical Science & Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang Key Laboratory of Green, Low-Carbon, and Efficient Development of Marine Fishery Resources, Zhejiang University of Technology (ZJUT), Hangzhou 310014, China.
Article Synopsis
- The actinomycete genus has a wide range of biosynthetic enzymes that can help in pollutant breakdown, chemical reactions, and discovering new natural products.
- A detailed analysis revealed that 86.5% of gene cluster families are unique to a specific phylogenomic clade, primarily focusing on non-ribosomal peptide synthetases (NRPS) and ribosomally synthesized peptides (RiPPs).
- The study identified several clade-specific novel RiPPs with antibacterial properties and noted that a marine strain generates new compounds when exposed to certain triggers, emphasizing the potential for discovering unique metabolites from this genus.
Targeting Tuberculosis: Novel Scaffolds for Inhibiting Cytochrome Oxidase.
J Chem Inf Model
July 2024
Department of Chemistry and Biochemistry, University of California, San Diego, La Jolla, California 92093, United States.
Discovered in the 1920s, cytochrome is a terminal oxidase that has received renewed attention as a drug target since its atomic structure was first determined in 2016. Only found in prokaryotes, we study it here as a drug target for (). Most previous drug discovery efforts toward cytochrome have involved analogues of the canonical substrate quinone, known as Aurachin D.
View Article and Find Full Text PDFAurachins, Bacterial Antibiotics Interfering with Electron Transport Processes.
Antibiotics (Basel)
June 2023
Laboratory of Technical Biology, Department of Biochemical and Chemical Engineering, TU Dortmund University, 44227 Dortmund, Germany.
Aurachins are farnesylated quinolone alkaloids of bacterial origin and excellent inhibitors of the respiratory chain in pro- and eukaryotes. Therefore, they have become important tool compounds for the investigation of electron transport processes and they also serve as lead structures for the development of antibacterial and antiprotozoal drugs. Especially aurachin D proved to be a valuable starting point for structure-activity relationship studies.
View Article and Find Full Text PDFBiocatalytic production of the antibiotic aurachin D in Escherichia coli.
AMB Express
November 2022
Department of Biochemical and Chemical Engineering, TU Dortmund University, Dortmund, Germany.
Aurachin D is a potent inhibitor of cytochrome bd oxidases, which are potential targets in the treatment of infectious diseases. In this study, our aim was to improve the biocatalytic production of aurachin D from a quinolone precursor molecule with recombinant Escherichia coli cells expressing the biosynthesis enzyme AuaA. In order to achieve a high-level production of this membrane-bound farnesyltransferase in E.
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