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    • 76. 发明公开
    • 2-Alkylthiopenem derivatives
    • 2-烷硫基青霉烯衍生物
    • EP0130025A1
    • 1985-01-02
    • EP84304083.3
    • 1984-06-18
    • PFIZER INC.
    • Hamanaka, Ernest Seiichi
    • C07D499/00A61K31/43
    • C07F7/186C07C327/00C07D333/32C07D333/34C07D333/48C07D335/02C07D499/88
    • 2-alkylthio-2-penem-3- carboxylic acid compounds, useful as antibacterials for treating mammals, have the formula:
      or a pharmaceutically acceptable salt thereof, wherein:

      R is 2-(methylsulfinyl) ethyl, 2-(methylsulfonyl)- ethyl, (methylsulfinyl)methyl, (methylsulfonyl)methyl, 3-thietanyl, 1-oxo-3-thietanyl, 1,1-dioxo-3-thietanyl, 2-thiolanyl, 1-oxo-2-thiolanyl, 3-thiolanyl, 1-oxo-3-thiolanyl, 1,1-dioxo-3-thiolanyl, 3-hydroxy-4-thiolanyl, 1-oxo-3-hydroxy-thiolanyl, 1, 1-dioxo-3-hydroxy-4-thiolanyl, 2-oxo-1, 3-dithiolan, 4-ylmethyl, 3-thianyl, 1-oxo-3-thianyl, 1, 1-dioxo-3-thianyl, 4-thianyl, 1-oxo-4-thianyl, 1, 1-dioxo-4-thianyl, 3-oxo-perhydro-1, 4-thiazin-2-yl. 4-formylperhydro-1, 4-thiazin-2-yl, 4-oxo-1, 4-oxathian-3-yl, 4, 4-dioxo-1, 4-oxathian-3-yl, 1, 3-dithiolan-2-yl, 1, 2-dithiolan-4-yl, or (2-methyl-3, 3-dioxo-1, 3-oxathiolan-5-yl) methyl; and
      R, is hydrogen or a group which forms an ester which is hydrolyzed in vivo.
    • 2-烷硫基-2-青霉烯-3-羧酸化合物,可用作治疗哺乳动物的抗细菌剂,具有下式:或其药学上可接受的盐,其中:R是2-(甲基亚磺酰基)乙基,2-(甲基磺酰基)乙基 ,(甲基亚磺酰基)甲基,(甲基磺酰基)甲基,3-硫杂环丁基,1-氧代-3-硫杂环丁基,1,1-二氧代-3-硫杂环丁烷基,2-硫代丙氨酰基,1-氧代-2-硫代丙酰基,3-硫代丙酰基, 3-氧代-3-硫代丙氨酰基,1,1-二氧代-3-硫代丙氨酰基,3-羟基-4-硫代丙氨酰基,1-氧代-3-羟基硫代丙酰基,1,1-二氧代-3-羟基-4-硫代丙氨酰基,2 - 氧代-1,3-二硫戊环,4-基甲基,3-硫烷基,1-氧代-3-硫烷基,1,1-二氧代-3-硫烷基,4-硫烷基,1-氧代-4-硫烷基,1,1 - 二氧代-4-硫烷基,3-氧代 - 全氢-1,4-噻嗪-2-基。 4-甲酰基全氢-1,4-噻嗪-2-基,4-氧代-1,4-氧硫杂环戊烷-3-基,4,4-二氧代-1,4-氧硫杂环戊烷-3-基,1,3-二硫戊环-2-基, 1,2-二硫戊环-4-基或(2-甲基-3,3-二氧代-1,3-氧硫杂环戊烷-5-基)甲基; R 1是氢或形成在体内水解的酯的基团。