Rapamycin analogs with reduced systemic exposure

Bioorg Med Chem Lett. 2005 Dec 1;15(23):5340-3. doi: 10.1016/j.bmcl.2005.06.106. Epub 2005 Sep 26.

Abstract

The synthesis and biological activities of rapamycin (I) analogs modified at the C-40 position are reported. Emphasis placed on compounds that potentially have an improved safety profile on account of their shorter in vivo half-life when compared with rapamycin.

MeSH terms

  • Animals
  • Antirheumatic Agents / chemistry*
  • Antirheumatic Agents / pharmacokinetics*
  • Antirheumatic Agents / toxicity
  • Arthritis, Rheumatoid / diagnostic imaging
  • Arthritis, Rheumatoid / drug therapy
  • Arthritis, Rheumatoid / metabolism*
  • Male
  • Radiography
  • Rats
  • Rats, Inbred Lew
  • Rats, Sprague-Dawley
  • Sirolimus / analogs & derivatives*

Substances

  • Antirheumatic Agents
  • Sirolimus