Synthesis of ramariolide natural products and discovery of their targets in mycobacteria

نویسندگان

  • Johannes Lehmann
  • Johannes Richers
  • Alexander Pöthig
  • Stephan A. Sieber
چکیده

Ramariolides A–D are natural products with antibacterial activity. To exploit their cellular mechanism, we here devise the first total synthesis and prepare a photoprobe for target identification. Antibacterial testing against several pathogenic strains includingMycobacterium tuberculosis revealed the highest potency for ramariolide A. Chemical proteomics unraveled binding to essential proteins for amino acid anabolism.

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منابع مشابه

Synthesis of ramariolide natural products and discovery of their targets in mycobacteria† †Electronic supplementary information (ESI) available. CCDC 1508942 and 1508943. For ESI and crystallographic data in CIF or other electronic format see DOI: 10.1039/c6cc08365j Click here for additional data file. Click here for additional data file.

Ramariolides A-D are natural products with antibacterial activity. To exploit their cellular mechanism, we here devise the first total synthesis and prepare a photoprobe for target identification. Antibacterial testing against several pathogenic strains including Mycobacterium tuberculosis revealed the highest potency for ramariolide A. Chemical proteomics unraveled binding to essential protein...

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Assessment of "drug-likeness" of a small library of natural products using chemoinformatics

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تاریخ انتشار 2016