硝基咪唑类抗结核药物结构修饰研究策略

Strategies for Structural Modification of Nitroimidazole Antituberculosis Drugs

结核病现已成为全球第二大致死疾病,虽然目前结核病的发生率呈现缓慢下降趋势,但耐药结核及耐多药结核仍是严重威胁人类健康的疾病.近年来,以PA-824,OPC-67683为代表的硝基咪唑类药物对结核杆菌尤其是耐多药结核杆菌表现出良好的抗菌活性.研究者进行了大量硝基咪唑化合物的构效关系研究,期望通过结构修饰改善其溶解性及安全性.综述了近年来硝基咪唑类化合物在抗结核领域的研究进展.

Tuberculosis has become the second leading disease that causes death in the world.Although the incidence of tuberculosis is decreasing slowly,drug-resistant tuberculosis and multi-drug-resistant tuberculosis are still the main threats.In recent years,the nitroimidazole drugs,such as PA-824 and OPC-67683,have shown good antimicrobial activity against Mycobacterium tuberculosis,especially against multidrug-resistant Mycobacterium tuberculosis.In the aim of improving the solubility and the safety of compounds,researchers have made extensive investigations into the structure-activity relationship of nitroimidazole compounds through structural modification.In this paper,the recent progress of nitroimidazole compounds that are used in anti-tuberculosis is reviewed.