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ChemInform Abstract: A New Series of Selective COX-2 Inhibitors: 5,6-Diarylthiazolo(3,2-b)( 1,2,4)triazoles.

✍ Scribed by P. ROY; Y. LEBLANC; R. G. BALL; C. BRIDEAU; C. C. CHAN; N. CHAURET; W. CROMLISH; D. ETHIER; J. Y. GAUTHIER; R. GORDON; G. GREIG; J. GUAY; S. KARGMAN; C. K. LAU; G. O'NEILL; J. SILVA; M. THERIEN; C. VAN STADEN; E. WONG; L. XU; P. PRASIT

Publisher
John Wiley and Sons
Year
2010
Weight
32 KB
Volume
28
Category
Article
ISSN
0931-7597

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✦ Synopsis

Diarylthiazolo(3,2b)

( 1,2,4)triazoles.

-Sixteen title compounds such as (I) are prepared for evaluation of potency and selectivity against human COX-1 and COX-2 enzymes. Most of the analogues in the series are very potent against the COX-2 enzyme. All of the compounds exhibit good selectivity in the COX-2 human whole blood assay. Compound (Ia) is the most potent and a selective oral COX-2 inhibitor. Furthermore, this compound demonstrates excellent pharmacokinetic and metabolic properties.

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