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Synthesis and biological evaluation of truncated derivatives of abyssomicin C as antibacterial agents.

Leticia MonjasPeter FodranJohanna KollbackCarlo CassaniThomas OlssonMaja GenhedenD G Joakim LarssonCarl-Johan Wallentin
Published in: Beilstein journal of organic chemistry (2019)
The synthesis and antibacterial activity of two new highly truncated derivatives of the natural product abyssomicin C are reported. This work outlines the limits of structural truncation of the natural product and consequently provides insights for further structure-activity relationship studies towards novel antibiotics targeting 4-amino-4-deoxychorismate (ADC) synthase. Specifically, it is demonstrated that the synthetically challenging bicyclic motif is essential for activity towards methicillin-resistant Staphylococcus aureus (MRSA).
Keyphrases
  • methicillin resistant staphylococcus aureus
  • structure activity relationship
  • staphylococcus aureus
  • silver nanoparticles
  • magnetic resonance imaging
  • wound healing