吡罗昔康，一种在细胞培养中前列腺素生成的强效抑制剂。构效关系研究。
Piroxicam, a potent inhibitor of prostaglandin production in cell culture. Structure-activity study.
作者信息
Carty T J, Eskra J D, Lombardino J G, Hoffman W W
出版信息
Prostaglandins. 1980 Jan;19(1):51-9. doi: 10.1016/0090-6980(80)90153-7.
The new non-steroidal antiinflammatory (NSAI)2 agent, piroxicam [4-hydroxy-2-methyl-N-(2-pyridyl)-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide], is a highly active inhibitor of prostaglandin (PG) synthesis by methylcholanthrene transformed mouse fibroblasts (MC5-5) and rabbit synovial cells in culture. Comparison of the PG biosynthesis inhibitory activity of piroxicam with other NSAI drugs in these experiments ranks piroxicam as among the most potent agents of this type now known. Some specific modifications of piroxicam's structure result in significant loss in PG synthesis blocking activity.
新型非甾体抗炎药（NSAI）2 吡罗昔康[4-羟基-2-甲基-N-(2-吡啶基)-2H-1,2-苯并噻嗪-3-甲酰胺 1,1-二氧化物]是一种高效的前列腺素（PG）合成抑制剂，可抑制经甲基胆蒽转化的小鼠成纤维细胞（MC5-5）和培养的兔滑膜细胞中的 PG 合成。在这些实验中，将吡罗昔康与其他 NSAI 药物的 PG 生物合成抑制活性进行比较，结果显示吡罗昔康是目前已知的这类药物中最有效的药物之一。吡罗昔康结构的某些特定修饰会导致 PG 合成阻断活性显著丧失。
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