Total synthesis and antimicrobial activity of +/--laurelliptinhexadecan-1-one and +/--laurelliptinoctadecan-1-one

Molecules. 2008 Nov 28;13(12):2935-47. doi: 10.3390/molecules13122935.

Abstract

The structures previously assigned to (+)-laurelliptinhexadecan-1-one (1a) and (+)-laurelliptinoctadecan-1-one (1b) from Cocculus orbiculatus (L.) DC. (Menispermaceae) have been confirmed by total synthesis of the racemic alkaloids. The key step of the synthesis involved formation of ring C of the aporphines by a radical-intiated cyclisation. Both (+/-)-laurelliptinhexadecan-1-one (1a) and (+/-)-laurelliptinoctadecan-1-one (1b) were inactive against Staphylococcus aureus ATCC25932, Escherichia coli ATCC10536 and Candida albicans ATCC90028.

MeSH terms

  • Anti-Infective Agents / chemical synthesis*
  • Anti-Infective Agents / chemistry
  • Anti-Infective Agents / pharmacology*
  • Candida albicans / drug effects
  • Cell Line, Tumor
  • Cocculus / chemistry
  • Escherichia coli / drug effects
  • Heterocyclic Compounds, 4 or More Rings / chemical synthesis*
  • Heterocyclic Compounds, 4 or More Rings / chemistry
  • Heterocyclic Compounds, 4 or More Rings / pharmacology*
  • Humans
  • Magnetic Resonance Spectroscopy
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Spectrophotometry, Ultraviolet
  • Staphylococcus aureus / drug effects
  • Stereoisomerism

Substances

  • Anti-Infective Agents
  • Heterocyclic Compounds, 4 or More Rings
  • laurelliptinhexadecan-1-one
  • laurelliptinoctadecan-1-one