AI Article Synopsis
- - The COX-2 inhibitor DFP has a long half-life in humans, indicating it stays in the body for an extended period.
- - Researchers are developing analogues of DFP to improve its pharmacokinetic properties, leading to enhanced effectiveness.
- - One notable analogue, 5(S)-(5-ethyl-5-methyl-3-(2-propoxy)-4-methanesulfonylphenyl)-2(5H)-furanone, is identified as a potent COX-2 inhibitor but is metabolized more quickly than DFP, suggesting a potentially shorter half-life in humans.
Article Abstract
The COX-2 inhibitor DFP [5,5-dimethyl-3-(2-propoxy)-4-methanesulfonylphenyl)-2(5H)-furanone] was found to have a long half-life in humans. Analogues have been characterized in order to optimize pharmacokinetics. This has lead to the discovery of 5(S)-(5-ethyl-5-methyl-3-(2-propoxy)-4-methanesulfonylphenyl)-2(5H)-furanone analogue 11 a potent and selective COX-2 inhibitor which is metabolized to a greater extent than DFP upon incubation with rat and human hepatocytes, suggesting a shorter half-life in humans.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/s0960-894x(02)00739-4 | DOI Listing |
Publication Analysis
Top Keywords
cox-2 inhibitor
12
potent selective
8
selective cox-2
8
half-life humans
8
discovery potent
4
inhibitor alkoxy
4
alkoxy lactone
4
lactone series
4
series optimized
4
optimized metabolic
4
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!