Record number :
792659
Title of article :
Discovery of a potent and selective COX-2 inhibitor in the alkoxy lactone series with optimized metabolic profile
Author/Authors :
Yves Leblanc، نويسنده , , Patrick Roy، نويسنده , , Zhaoyin Wang، نويسنده , , Chun-Sing Li، نويسنده , , Nathalie Chauret، نويسنده , , Deborah A. Nicoll-Griffith، نويسنده , , Jose M. Silva، نويسنده , , Yves Aubin، نويسنده , , James A. Yergey، نويسنده , , Chi-Chung Chan، نويسنده , , Denis Riendeau، نويسنده , , Christine Brideau، نويسنده , , Robert Gordon، نويسنده , , Lijing Xu، نويسنده , , Janine Webb، نويسنده , , Denise M. Visco، نويسنده , , Petpiboon Prasit، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2002
Pages :
4
From page :
3317
To page :
3320
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.
Journal title :
Bioorganic & Medicinal Chemistry Letters
Journal title :
Bioorganic & Medicinal Chemistry Letters
Serial Year :
2002
Link To Document :
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