Effect of 2,4-disubstituted thiazol-5yl-aminoketones on inflammation. In vitro and in vivo biological studies: a structure-activity approach.

Some modified novel thiazol-5yl-aminoketones were evaluated for their anti-inflammatory, analgesic and antiproteolytic activities. Their inhibitory activity on 12-lipoxygenase (12-LO) and beta-glucuronidase in vitro was estimated. Their interaction with the stable free radical 1,1-diphenyl-2-picrylhydrazyl (DPPH) and their RM values were also determined. For two of them, the effect on zoxazolamine-induced paralysis after a prolonged treatment was determined. The duration of paralysis for the same compounds, (only one administration, one before zoxazolamine injection) was recorded too. The 2-amino substituted derivatives seem to be more potent in comparison with the 2-phenyl. The tested compounds were found to influence proteolysis but not the activities at beta-glucuronidase and 12-LO. Their interaction with DPPH was mild. Compound 2 seems to modify the activity of the hepatic drug metabolizing enzymes. In conclusion, their activity is related to certain structural characteristics.
AuthorsD J Hadjipavlou-Litina, A A Geronikaki
JournalResearch communications in molecular pathology and pharmacology (Res Commun Mol Pathol Pharmacol) Vol. 96 Issue 3 Pg. 307-18 (Jun 1997) ISSN: 1078-0297 [Print] UNITED STATES
PMID9261890 (Publication Type: Journal Article)
Chemical References
  • Analgesics
  • Anti-Inflammatory Agents, Non-Steroidal
  • Enzyme Inhibitors
  • Ketones
  • Lipoxygenase Inhibitors
  • Zoxazolamine
  • Glucuronidase
  • Analgesics (pharmacology)
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal (pharmacology)
  • Drug Synergism
  • Enzyme Inhibitors (pharmacology)
  • Female
  • Glucuronidase (antagonists & inhibitors)
  • Ketones (chemistry, pharmacology)
  • Lethal Dose 50
  • Lipoxygenase Inhibitors
  • Male
  • Mice
  • Mice, Inbred AKR
  • Microsomes, Liver (drug effects, enzymology)
  • Rats
  • Rats, Wistar
  • Structure-Activity Relationship
  • Zoxazolamine (metabolism, pharmacology)

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