Pyrido[4,3-e]-1,2-thiazine-3-carboxamide 誘導体の合成と抗炎症作用(メディシナルケミストリー)
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A series of 3-carboxamides of pyrido[4,3-e]-1,2-thiazine was synthesized and evaluated for antiinflammatory activity in carrageenin rat paw edema. These compounds were prepared by cyclization of N-(substituted carbamoylmethyl)-4-methoxycarbonyl-N-methylpyridine-3-sulfonamides in the presence of sodium methoxide. Some of them were prepared alternatively by aminolysis of pyrido[4,3-e]-1,2-thiazine-3-carboxylic ester with aryl- and heteroarylamines. Among the compounds tested, N-phenyl- and N-(2-pyridyl)-carboxamides showed a potent antiinflammatory activity and a weaker action in causing gastrointestinal lesions than that of the reference drug, piroxicam.
- 公益社団法人日本薬学会の論文
- 1986-11-25
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- Pyrido[4,3-e]-1,2-thiazine-3-carboxamide 誘導体の合成と抗炎症作用(メディシナルケミストリー)