Abstract |
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.
|
Authors | D J Hadjipavlou-Litina, A A Geronikaki |
Journal | Research 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 |
PMID | 9261890
(Publication Type: Journal Article)
|
Chemical References |
- Analgesics
- Anti-Inflammatory Agents, Non-Steroidal
- Enzyme Inhibitors
- Ketones
- Lipoxygenase Inhibitors
- Zoxazolamine
- Glucuronidase
|
Topics |
- 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)
|