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