The history of incessant struggle and the current global burden associated with emerging infectious disease especially tuberculosis, guided us to define the scope of this research project, and to identify research gaps in synthesizing some heterocyclic compounds for anti-tubercular activity. In this research project, we have synthesized a series of novel heterocyclic (benzothiazoles) compounds viz N'-((1-(7-chloro-6-fluorobenzo[d]thiazol-2-yl)-3-phenyl-1H-pyrazol-4-yl) methylene)isonicotinohydrazide 12a-c their 5-nitro 15a-c and 4-nitro 18a-c derivatives, by a series of reactions of their respective synthons. The completion of reaction and the purity of the synthesized compounds have been established by chromatographic analysis. All the newly synthesized compounds satisfactorily show acceptable analysis for their anticipated structures, which have been confirmed based on physicochemical and spectral data. These newly synthesized compounds have been primarily evaluated for their in vitro anti-tubercular activity by Ziehl-Neelsen stain method. Compounds 15a, 15b, 15c, 18b and 18c have shown 100% inhibition at 25 mg/ mL and MIC values of around 45 nM against M. tuberculosis H₃₇Rv (ATCC 27294). Cytotoxicity on THP-1 cell line shows that all the tested compounds are safe.

中文翻译：

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苯并噻唑并吡唑并异烟肼衍生物的合成及其硝基区域异构体的抗结核活性

不断的奋斗历史以及当前与新兴传染病（尤其是结核病）相关的全球负担，引导我们定义了该研究项目的范围，并确定了在合成一些用于抗结核活性的杂环化合物方面的研究差距。在本研究项目中，我们已经合成了一系列新的杂环（苯并噻唑）的化合物即 N” - （（1-（7-氯-6-氟苯并[ d ]噻唑-2-基）-3-苯基- 1 H ^ -吡唑-4-基）亚甲基）异二十二酰肼12a-c及其5-硝基15a-c和4-硝基18a-c衍生物，通过它们各自的合成子的一系列反应。通过色谱分析已经确定了反应的完成和所合成化合物的纯度。所有新合成的化合物均令人满意地显示出其预期结构的可接受的分析，这些分析已基于理化和光谱数据得到证实。这些新合成的化合物已通过Ziehl-Neelsen染色法初步评估了其体外抗结核活性。化合物15a，15b，15c，18b和18c在25 mg / mL时对结核分枝杆菌H ₃₇表现出100％的抑制作用，MIC值约为45 nM 。Rv（ATCC 27294）。对THP-1细胞系的细胞毒性表明，所有测试的化合物都是安全的。