Thiazolidin-4-one scaffold has great potential for medicinal chemistry and is of interest to scientists in view of wide spectrum of biological activity. This scaffold is often used for designing of small molecules with various biological activity including antituberculosis activity. The presented review is an attempt to gather, analyze and systemize data about antitubercular properties of thiazolidine-4-ones from two last decades. Some of them have promising antitubercular activity which is significantly higher than that of the reference drugs. Among them compounds 82c, 82d and 84 that were active against M. tuberculosis H37Rv strain with MICs in the range of 0.05–0.2 μg/mL and compound 108 exhibited activity with MIC = 0.36 μM. Compounds 115a-115c and 116a-116c were very effective against M. tuberculosis H37Ra with MIC values in the range of 0.031–0.125 μg/mL. Acidomycin was showed activity against seven MDR M. tuberculosis strains with MICs in the range of 0.6–0.62 μM and against two XDR M. tuberculosis strains with MICs 0.096 and 1.2 μM. The structure-activity relationship (SAR) of some groups of compounds, as well as some potential molecular targets were also discussed.

噻唑烷-4-酮支架在药物化学中具有巨大潜力，并且鉴于其广泛的生物活性，因此引起了科学家的兴趣。该支架通常用于设计具有各种生物活性，包括抗结核活性的小分子。提出的评论是试图收集，分析和系统化最近20年间有关噻唑烷4-one的抗结核特性的数据。它们中的一些具有有希望的抗结核活性，其显着高于参考药物的抗结核活性。其中化合物82c，82d和84具有MICs在0.05-0.2μg/ mL范围内对结核分枝杆菌H37Rv菌株有活性，以及化合物108MIC = 0.36μM时显示出活性。化合物115a-115c和116a-116c对结核分枝杆菌H37Ra非常有效，MIC值为0.031-0.125μg/ mL。酸性霉素对具有MIC范围为0.6–0.62μM的7株MDR结核菌和具有MIC为0.096和1.2μM的2种XDR结核菌均具有活性。还讨论了一些化合物的结构-活性关系（SAR），以及一些潜在的分子靶标。