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吡罗昔康代谢产物的合成与抗炎活性

Synthesis and antiinflammatory activity of metabolites of piroxicam.

作者信息

Lombardino J G

出版信息

J Med Chem. 1981 Jan;24(1):39-42. doi: 10.1021/jm00133a009.

Abstract

Four possible pyridine monohydroxylated metabolites of the antiinflammatory agent piroxicam have been synthesized for comparison with a natural pyridine-hydroxylated metabolite of this compound. In addition, another metabolite of piroxicam, derived from dehydration of the parent drug, has been made and characterized. The antiinflammatory activity of these compounds and four other known metabolites of piroxicam has been measured in the carrageenan-induced rat paw edema model and all are found to be less active than piroxicam itself.

摘要

已合成了抗炎药吡罗昔康的四种可能的吡啶单羟基化代谢物,用于与该化合物的一种天然吡啶羟基化代谢物进行比较。此外,还制备并表征了吡罗昔康的另一种由母体药物脱水衍生而来的代谢物。已在角叉菜胶诱导的大鼠足爪水肿模型中测定了这些化合物以及吡罗昔康的其他四种已知代谢物的抗炎活性,结果发现它们的活性均低于吡罗昔康本身。

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