Tuberculosis is one of major health problems worldwide. Approximately 1.8 mil ion people died from Tuberculosis each year which has become a global public health issue. Recently the emergence of drug resistant strains and HIV co-infection has resulted in a high incidence. As a result, there is an urgent need for us to understand the resistance mechanism and discover new anti-tuberculosis drugs. A number of new potential anti-tuberculosis drug candidates with novel modes of action have entered clinical trials in recent years. These agents are most likely to be effective against resistant strains. The paper summarized structure-activity relationships, in vitro and in vivo activity, pharmacokinetics, mechanism of action and combination regimens about several novel anti-tuberculosis drugs.% 结核病(Tuberculosis)是世界范围里的主要疾病之一，近年来，每年约有180万人死于结核病，结核病已经成为全球性的公众健康问题。近年来药物耐受以及伴有 HIV 感染的结核病发病率急剧增加，迫切需要深入了解目前抗结核药物的作用机制及耐药机制，以指导开发对持留菌和耐药菌更加有效的新型药物。近年来，一批具有全新作用机制的抗结核候选药物相继进入了临床研究，并且这些药物对耐药株表现出有效的抑制活性。文章对几类新型抗结核药物的化学结构、作用机制、构效关系、抗结核活性以及临床应用进行了综述。
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