Synthesis and Anti-inflammatory Activity of Steroidal 17-Yl-α-Oxothiocarboxamides and Related Compounds

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概要

• 論文の詳細を見る

• The Willgerodt-Kindler reaction of 21-chloro-20-ketosteroids (5) or sodium 21-thiosulfate derivatives of 20-ketosteroids (6) with sulfur in secondary amines gave the corresponding steroidal α-oxothiocarboxamides (3) in good yields. Among these compounds (3), 11β, 17α-dihydroxy-21-morpholinopregna-1,4-diene-3,20-dione-21-thione (3a) and 11β, 17α-dihydroxy-21-morpholinopregn-4-ene-3,20-dione-21-thione (3b) showed potent anti-inflammatory activities comparable to or a little less than those of the parent compounds, prednisolone and hydrocortisone, respectively, in the carrageenin edema test in rats. 3a also showed potent activity in the granuloma pouch test in rats but much less activity in the cotton pellet test in rats. These results suggest that 3a might be more active against acute or subacute inflammation than against chronic inflammation.

• 社団法人日本薬学会の論文
• 1979-06-25

著者

• 野口 俊作

  Central Research Division, Takeda Chemical Industries, Ltd.

• 大林 幹彦

  Central Research Division, Takeda Chemical Industries, Ltd.

• 野口 俊作

  Central Research Division Takeda Chemical Industries Ltd.

• 大林 幹彦

  Central Research Division Takeda Chemical Industries Ltd.

• 葛声 成二

  Central Research Division, Takeda Chemical Industries, Ltd.

• 葛声 成二

  武田薬品中央研究所

• 葛声 成二

  Medicinal Research Laboratories Central Research Division Takeda Chemical Industries Ltd.

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