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    Halogenated antituberculosis agents
    7.
    发明授权
    Halogenated antituberculosis agents 失效
    卤化抗结核药

    公开(公告)号：US06624153B2

    公开(公告)日：2003-09-23

    申请号：US10237416

    申请日：2002-09-09

    申请人： Farzad Kobarfard ,  Joel M. Kauffman

    发明人： Farzad Kobarfard ,  Joel M. Kauffman

    IPC分类号： C07C31195

    CPC分类号： C07C281/14 ,  C07C337/08

    摘要： Halogenated derivatives of two synthetic anti-tuberculosis agents, thioacetazone and p-aminosalicylic acid, have been synthesized. In general, the halogenated compound has the structure of Structure I: wherein X1 is a halogen and X2 is a second halogen or hydrogen, and Y is sulfur or oxygen; or, has the structure of Structure IV: wherein X1 is a halogen and X2 is a second halogen or hydrogen. Alternatively, the halogenated compounds may be pharmaceutically acceptable salts of these compounds. These halogenated derivatives possess anti-mycobacterial activity and are particularly useful for the treatment of Mycobacterium tuberculosis infections. In particular, fluorinated analogs of thioacetazone and p-amino-salicylic acid have been synthesized for use as anti-tuberculosis therapeutic agents either alone or in combination with other conventional anti-tuberculosis therapeutic agents.

    摘要翻译： 已经合成了两种合成抗结核药物硫代乙酮和对氨基水杨酸的卤代衍生物。 通常，卤代化合物具有结构I的结构：其中X1是卤素，X2是第二个卤素或氢，Y是硫或氧; 或具有结构IV的结构：其中X1是卤素，X2是第二个卤素或氢。 或者，卤化化合物可以是这些化合物的药学上可接受的盐。 这些卤代衍生物具有抗分枝杆菌活性，特别可用于治疗结核分枝杆菌感染。 特别地，已经合成硫代乙酮和对氨基水杨酸的氟化类似物单独使用或与其它常规抗结核治疗剂组合用作抗结核治疗剂。