Synthesis and antimicrobial activity of N-analogous corollosporines

Org Biomol Chem. 2006 Apr 7;4(7):1365-75. doi: 10.1039/b517101f. Epub 2006 Feb 28.

Abstract

Corollosporine is an antimicrobial metabolite, which was isolated from the marine fungus Corollospora maritima. Owing to its basic 4-hydroxyphthalic acid anhydride structure, it has become an attractive target for a structure/activity relationship modelling of derived compounds with potential antibiotic activity. In this regard we report on the straightforward synthesis of hetero analogous corollosporines, which were easily prepared by a three-step reaction sequence, taking advantage of a novel multicomponent reaction (AAD-reaction) and a subsequent aromatization/Grignard reaction protocol. Furthermore, the obtained products were tested in several biological assays to evaluate their antimicrobial activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Bacillus subtilis / drug effects
  • Escherichia coli / drug effects
  • Magnetic Resonance Spectroscopy
  • Microbial Sensitivity Tests
  • Models, Molecular
  • Molecular Conformation
  • Phthalic Anhydrides / chemical synthesis*
  • Phthalic Anhydrides / chemistry
  • Phthalic Anhydrides / pharmacology*
  • Staphylococcus aureus / drug effects
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Phthalic Anhydrides
  • corollosporine