Synthesis and biological evaluation of novel cyclosporin a analogues: potential soft drugs for the treatment of autoimmune diseases

J Med Chem. 2003 Feb 27;46(5):674-6. doi: 10.1021/jm025595i.

Abstract

Cyclosporin A is effective in the treatment of asthma patients, but its chronic use is limited by toxicity. Novel cyclosporin A analogues were synthesized utilizing the olefin metathesis reaction and evaluated in a calcineurin A inhibition assay. The novel analogues demonstrated activity comparable to activity of the parent molecule and are potential soft drugs.

MeSH terms

  • Autoimmune Diseases / drug therapy
  • Calcineurin Inhibitors
  • Cyclosporins / chemical synthesis*
  • Cyclosporins / chemistry
  • Immunosuppressive Agents / chemical synthesis*
  • Immunosuppressive Agents / chemistry
  • Structure-Activity Relationship

Substances

  • Calcineurin Inhibitors
  • Cyclosporins
  • Immunosuppressive Agents