Based on bioisosteric similarities with thiacetazone, a series of 7-chloro-4-aminoquinoline derivatives have been designed and synthesized. The target compounds were elucidated by NMR, mass, and FTIR spectral data. All synthesized compounds were evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv (MTB), and human dermal fibroblast cell lines were used to assess toxicity of selected ligands. All of the designed compounds showed inhibition of MTB with MIC of 1.56–50 μM. Among the tested compounds, 7c and 7g proved to be most potent MTB inhibitors (MIC = 1.56 μM). The outcome of present study suggests that most of the synthesized compounds are sensitive to Mycobacterium tuberculosis and showed acceptable range for molecular parameters. Thus, 7-chloro-4-aminoquinolines could be a useful lead for the development of new MTB inhibitory agents.

中文翻译：

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一些4-氨基喹啉衍生物作为潜在的抗结核药物的合成及生物学评价

基于与噻乙zone的生物立体相似性，设计并合成了一系列7-氯-4-氨基喹啉衍生物。通过NMR，质量和FTIR光谱数据阐明了目标化合物。评估所有合成的化合物对结核分枝杆菌H37Rv（MTB）的体外抗结核活性，并使用人皮肤成纤维细胞系评估所选配体的毒性。所有设计的化合物均显示出对MTB的抑制作用，MIC为1.56–50μM。在测试的化合物中，7c和7g被证明是最有效的MTB抑制剂（MIC = 1.56μM）。本研究的结果表明，大多数合成的化合物对结核分枝杆菌敏感，并显示出可接受的分子参数范围。从而，