Synthesis of the Cyanobacterial Antibiotics Anaephenes A and B

J Nat Prod. 2020 Jun 26;83(6):2036-2040. doi: 10.1021/acs.jnatprod.0c00279. Epub 2020 May 26.

Abstract

The first syntheses of the antibacterial natural products anaephenes A (1) and B (2) are reported. Both natural products were synthesized in five linear steps from commercially available tert-butyl(3-iodophenoxy)dimethylsilane. Key steps for the synthesis included a Sonogashira cross-coupling and a Julia-Kocienski olefination to selectively construct the E-alkene present in the natural products. This synthetic route allowed the identities and antimicrobial activities of anaephenes A (1) and B (2) to be confirmed. Additionally, these compounds displayed antimicrobial activity against methicillin-resistant Staphylococcus aureus (MRSA) with MIC values of 16 and 8 μg/mL, respectively.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Alkenes / chemical synthesis
  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / pharmacology
  • Cyanobacteria / chemistry*
  • Methicillin-Resistant Staphylococcus aureus / drug effects
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Phenols / chemical synthesis*
  • Phenols / pharmacology

Substances

  • Alkenes
  • Anti-Bacterial Agents
  • Phenols
  • anaephene A
  • anaephene B