Synthesis and characterization of novel indole derivatives reveal improved therapeutic agents for treatment of ischemia/reperfusion (I/R) injury.

To develop more potent therapeutic agents with therapeutic efficacy for ischemia/reperfusion (I/R) injury, we linked an antiinflammatory moiety (1,3-dioxane derivative) to the key pharmacophoric moiety of melatonin. We hypothesized that the resulting new indole derivatives might induce a synergistic protection against oxidative damage associated with I/R injury. Our results indicate that one of these indole derivatives (7) manifests potent antiinflammatory antioxidant effects and exerts a protective effect against skeletal muscle injury and associated lung injury following limb I/R in rats.
AuthorsWei Bi, Yue Bi, Ping Xue, Yanrong Zhang, Xiang Gao, Zhibo Wang, Meng Li, Michèle Baudy-Floc'h, Nathaniel Ngerebara, K Michael Gibson, Lanrong Bi
JournalJournal of medicinal chemistry (J Med Chem) Vol. 53 Issue 18 Pg. 6763-7 (Sep 23 2010) ISSN: 1520-4804 [Electronic] United States
PMID20731361 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, Non-P.H.S.)
Chemical References
  • Anti-Inflammatory Agents, Non-Steroidal
  • Antioxidants
  • Free Radical Scavengers
  • Indoles
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal (chemical synthesis, chemistry, pharmacology)
  • Antioxidants (chemical synthesis, chemistry, pharmacology)
  • Capillary Permeability
  • Free Radical Scavengers (chemical synthesis, chemistry, pharmacology)
  • Hindlimb (blood supply)
  • Indoles (chemical synthesis, chemistry, pharmacology)
  • Inflammation (drug therapy)
  • Lipid Peroxidation (drug effects)
  • Lung Injury (drug therapy, metabolism, pathology)
  • Mice
  • Muscle, Skeletal (blood supply, drug effects, pathology)
  • PC12 Cells
  • Rats
  • Reperfusion Injury (drug therapy, metabolism, pathology)
  • Structure-Activity Relationship

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research network!

Choose Username:
Verify Password: