Synthesis and biological properties of macrolactam analogs of the natural product macrolide (-)-A26771B

Bioorg Med Chem Lett. 2011 Aug 15;21(16):4768-72. doi: 10.1016/j.bmcl.2011.06.073. Epub 2011 Jun 23.

Abstract

Promising synthetic derivatives of macrolactone natural product (-)-A26771B have been designed and synthesized both from semisynthesis and total synthesis. Further optimization led to the first synthesis of macrolactam analogs of (-)-A26771B with improved antibacterial activity and metabolic stability.

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / metabolism
  • Anti-Bacterial Agents / pharmacology*
  • Bacteria / drug effects*
  • Biological Factors / chemical synthesis
  • Biological Factors / metabolism
  • Biological Factors / pharmacology*
  • Dose-Response Relationship, Drug
  • Drug Design
  • Lactones / chemical synthesis
  • Lactones / metabolism
  • Lactones / pharmacology
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Biological Factors
  • Lactones
  • A26771B