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:
1
wherein X
1
is a halogen and X
2
is a second halogen or hydrogen, and Y is sulfur or oxygen; or,
has the structure of Structure IV:
2
wherein X
1
is a halogen and X
2
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.
已经合成了两种合成抗结核药物
硫代乙酰唑和对
氨基
水杨酸的卤代衍
生物。一般来说,卤代化合物具有结构I:1的结构,其中X1是卤素,X2是第二个卤素或氢,Y是
硫或氧;或者,具有结构IV:2的结构,其中X1是卤素,X2是第二个卤素或氢。或者,这些卤代化合物可以是这些化合物的药物可接受的盐。这些卤代衍
生物具有抗分枝杆菌活性,特别适用于治疗结核分枝杆菌感染。特别是,已经合成了
硫代乙酰唑和对
氨基
水杨酸的
氟化类似物,用于作为抗结核治疗剂,单独使用或与其他常规抗结核治疗剂联合使用。