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

Abstract
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
Topics
  • 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

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