We prepared fifty various 9H‐fluorenone based 1,2,3‐triazole analogues varied with NH, –S–, and –SO₂– groups using click chemistry. The target compounds were characterized by routine analytical techniques, ¹H, ¹³CNMR, mass, elemental, single‐crystal XRD (8a) and screened for in vitro antitubercular activity against Mycobacterium tuberculosis (MTB) H37Rv strain and two “wild” strains Spec. 210 and Spec. 192 and MIC₅₀ was determined. Further, the compounds were evaluated for MTB InhA inhibition study as well. The final analogues exhibited minimum inhibitory concentration (MIC) ranging from 52.35 to >295 μm. Among the –NH– analogues, one compound 5p (MIC 58.34 μm), among –S– containing analogues four compounds 8e (MIC 66.94 μm), 8f (MIC 74.20 μm), 8g (MIC 57.55 μm), and 8q (MIC 56.11 μm), among –SO₂– containing compounds one compound 10p (MIC 52.35 μm) showed less than MTB MIC 74.20 μm: Compound 4‐(((9H‐fluoren‐9‐yl)sulfonyl)methyl)‐1‐(3,4,5‐trimethoxyphenyl)‐1H‐1,2,3‐triazole (10p) was found to be the most active compound with 73% InhA inhibition at 50 μm; it inhibited MTB with MIC 52.35 μm. Further, 10f and 10p were docked to crystal structure of InhA to know binding interaction pattern. Most active compounds were found to be non‐cytotoxic against HEK 293 cell lines at 50 μm.

中文翻译：

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设计和合成基于9H-芴酮的1,2,3-三唑类似物作为结核分枝杆菌InhA抑制剂

我们使用点击化学方法制备了50种不同的9 H-芴酮基1,2,3-三唑类似物，其中NH，–S–和–SO ₂ –组不同。通过常规分析技术，¹ H，¹³ CNMR，质量，元素，单晶XRD（8a）对目标化合物进行表征，并筛选出针对结核分枝杆菌（MTB）H37Rv菌株和两个“野生”菌株的体外抗结核活性。210和规格 192和MIC ₅₀被确定。此外，还对化合物进行了MTB InhA抑制研究。最终的类似物表现出的最小抑菌浓度（MIC）为52.35至> 295μ米。其中-NH-类似物，一种化合物5P（MIC 58.34μ米），其中含有-S-类似物四种化合物8E（MIC 66.94μ米），8F（MIC 74.20μ米），8克（MIC 57.55μ米），和8Q（MIC 56.11μ米），其中-SO ₂ -包含化合物的一种化合物10便士（MIC 52.35μ米）显示小于MTB MIC 74.20μ米：化合物4 - （（（9- ħ芴-9-基）磺酰基）甲基）-1-（3,4,5-三甲氧基苯基）-1 H -1,2,3-三唑（10p）被认为是在50μ73％抑制INHA最活跃的化合物米; 它抑制MTB与MIC 52.35μ米。此外，将10f和10p对接至InhA的晶体结构以了解结合相互作用模式。发现大多数活性化合物在50μ是针对HEK 293细胞系无细胞毒性的米。