Searching for new active molecules against M. Bovis BCG and Mycobacterium tuberculosis (MTB) H37Ra, a focused of 1,2,3-triazoles-incorporated 2,4 thiazolidinedione conjugates have been efficiently prepared via a click chemistry approach cyclocondensation of 4-amino-N-(5-methylisoxazol-3-yl)benzenesulfonamide (4), aryl aldehyde (5a–l), and mercapto acetic acid (6) with good to promising yields. The newly synthesized compounds were tested against drug-sensitive MTB and BCG. In particular, compounds 8g, 8h, 8j and 8l are highly potent against both the strains with IC₉₀ values in the range of 1.20–2.70 and 1.24–2.65 µg/mL, respectively. Based on the results from the antitubercular activity, SAR for the synthesized series has been developed. Most of the active compounds were non-cytotoxic against MCF-7, HCT 116 and A549 cell lines. Most active compounds were having a higher selectively index, which suggested that these compounds were highly potent.

为寻找针对牛分枝杆菌BCG和结核分枝杆菌（MTB）H37Ra的新活性分子，已通过点击化学方法通过4-氨基环戊基的环缩合反应，有效地制备了结合了1,2,3-三唑的2,4噻唑烷二酮共轭物。N-（5-甲基异恶唑-3-基）苯磺酰胺（4），芳基醛（5a–l）和巯基乙酸（6）具有良好的收率。测试了新合成的化合物对药物敏感的MTB和BCG的敏感性。特别是化合物8g，8h，8j和8l两种菌株的IC ₉₀值分别在1.20–2.70和1.24–2.65 µg / mL的范围内均具有很高的效力。基于抗结核活性的结果，已开发了合成系列的SAR。大多数活性化合物对MCF-7，HCT 116和A549细胞系均无细胞毒性。大多数活性化合物具有较高的选择性指数，这表明这些化合物非常有效。