N-Demethylation of nocathiacin I via photo-oxidation

Bioorg Med Chem Lett. 2008 Jul 15;18(14):4051-3. doi: 10.1016/j.bmcl.2008.05.112. Epub 2008 Jun 4.

Abstract

In order to improve aqueous solubility of nocathiacin I (1), a potent antibacterial agent, N-demethylation of the amino-sugar moiety was sought. Irradiation of 1 in DMF/CH(2)Cl(2) with UV light of 380 nm led to a cyclic product 2, which was hydrolyzed to yield the desired nocathiacin VI (3). Treatment of 1 with shorter UV light caused trans-cis isomerization of a c-c double bond.

MeSH terms

  • Anti-Infective Agents / pharmacology
  • Chemistry, Pharmaceutical / methods
  • Drug Design
  • Hydrolysis
  • Intercellular Signaling Peptides and Proteins
  • Light
  • Methylation
  • Models, Chemical
  • Molecular Structure
  • Oxidation-Reduction
  • Oxygen / chemistry*
  • Peptides / chemistry*
  • Solubility
  • Solvents / chemistry
  • Structure-Activity Relationship
  • Ultraviolet Rays

Substances

  • Anti-Infective Agents
  • Intercellular Signaling Peptides and Proteins
  • Peptides
  • Solvents
  • nocathiacin I
  • Oxygen