Antifungal rapamycin analogues with reduced immunosuppressive activity

Bioorg Med Chem Lett. 2000 Jul 3;10(13):1405-8. doi: 10.1016/s0960-894x(00)00184-0.

Abstract

Several 1,2,3,4-tetrahydro- and 7-N-hydroxycarbamate derivatives of the natural product rapamycin were prepared and assayed for their immunosuppressive and antifungal profiles. Substitutions at the 7-position indicate the possibility of a differentiated immunosuppressive to antifungal profile, whereas 40-position variants of the tetrahydro-analogues did not show similar differentiated activity.

MeSH terms

  • Animals
  • Antifungal Agents / chemistry
  • Antifungal Agents / pharmacology*
  • Biopharmaceutics
  • Candida / drug effects
  • Chemistry, Pharmaceutical
  • Humans
  • Immunosuppressive Agents / chemistry
  • Immunosuppressive Agents / pharmacology
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Signal Transduction
  • Sirolimus / analogs & derivatives*
  • Sirolimus / chemistry
  • Sirolimus / pharmacology*

Substances

  • Antifungal Agents
  • Immunosuppressive Agents
  • Sirolimus