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Synthesis and biological evaluation of phenyl-1H-1,2,3-triazole derivatives as anti-inflammatory agents.

Abstract
Rapid and efficient synthesis of a phenyl-1H-1,2,3-triazole library enabled cost-effective biological testing of a range of novel non-steroidal anti-inflammatory drugs with potential for improved drug efficacy and toxicity profiles. Anti-inflammatory activities of the phenyl-1H-1,2,3-triazole analogs synthesized in this report were assessed using the xylene-induced ear edema model in mice. At least four analogs, 2a, 2b, 2c, and 4a, showed more potent effects than the reference anti-inflammatory drug diclofenac at the same dose of 25 mg/kg. To explore relationships between the structural properties of phenyl-1H-1,2,3-triazole analogs and their anti-inflammatory activities in xylene-induced ear edema, comparative molecular field analysis was performed, and pharmacophores showing good anti-inflammatory activities were identified based on an analysis of contour maps obtained from comparative molecular field analysis. The anti-inflammatory effect on the molecular level was tested by the expression of tumor necrosis factor-alpha induced COX-2 using Western blots. Because the addition of the analog 2c caused the expression change of TNF-α induced COX-2, the molecular binding mode between 2c and COX-2 was elucidated using in silico docking.
AuthorsTae Woo Kim, Yeonjoong Yong, Soon Young Shin, Hyeryoung Jung, Kwan Ha Park, Young Han Lee, Yoongho Lim, Kang-Yeoun Jung
JournalBioorganic chemistry (Bioorg Chem) Vol. 59 Pg. 1-11 (Apr 2015) ISSN: 1090-2120 [Electronic] United States
PMID25658192 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2015 Elsevier Inc. All rights reserved.
Chemical References
  • Anti-Inflammatory Agents, Non-Steroidal
  • Triazoles
  • Tumor Necrosis Factor-alpha
  • Xylenes
  • Cyclooxygenase 2
Topics
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal (chemical synthesis, chemistry, therapeutic use)
  • Cyclooxygenase 2 (immunology)
  • Ear (pathology)
  • Edema (chemically induced, drug therapy, immunology, pathology)
  • Male
  • Mice
  • Molecular Docking Simulation
  • Molecular Structure
  • Structure-Activity Relationship
  • Triazoles (chemical synthesis, chemistry, therapeutic use)
  • Tumor Necrosis Factor-alpha (immunology)
  • Xylenes

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