Background: Pyrazole derivatives have been reported to possess numerous pharmacological activities viz., anti-inflammatory, antipsychotic, etc. Our group has disclosed that pyrazole benzamides display potent antibacterial and anti-tubercular activities.

Objective: Synthesis of new pyrazole acetamides which possess hydrazone group to be evaluated for antitubercular activity.

Methods: The key intermediate 5-aminopyrazole was synthesized with the known procedure, which is then converted into chloroacetamide. This compound than resulted in hydrazine derivative and finally converted into aromatic hydrazones. All the compounds were screened for antitubercular activity.

Results: All the synthesized compounds have been characterized by their spectral data obtained and subjected to anti-tubercular activity. Among all the twenty tested compounds, three compounds, 5a5, 5b5 and 5b7 have demonstrated MIC value of 3.12 μg/mL against MTB H37Rv. Docking studies revealed important hydrogen bonding interactions with InhA.

Conclusion: Three compounds 5a5, 5b5 and 5b7 were found to be most potent among the series of compounds. Docking studies of compounds explained the presence of hydrogen bonding and π- π stacking interactions with InhA. Further synthesis of more such derivatives with optimized groups would produce compounds with more potent anti-tubercular activity.

背景：吡唑衍生物据报道具有许多药理活性，即抗炎，抗精神病药等。我们的研究小组已披露，吡唑苯甲酰胺具有强大的抗菌和抗结核活性。

目的：合成具有基的新型吡唑乙酰胺，以评估其抗结核活性。

方法：采用已知方法合成了关键中间体5-氨基吡唑，然后将其转化为氯乙酰胺。然后该化合物产生肼衍生物，最后转化为芳族。筛选所有化合物的抗结核活性。

结果：所有合成的化合物均已通过获得的光谱数据进行了表征，并具有抗结核活性。在所有二十种测试化合物中，三种化合物5a5、5b5和5b7对MTB H37Rv的MIC值显示为3.12μg/ mL。对接研究显示与InhA的重要氢键相互作用。

结论：在这一系列化合物中，发现三种化合物5a5、5b5和5b7最有效。化合物的对接研究解释了氢键的存在以及与InhA的π-π堆积相互作用。具有优化基团的更多此类衍生物的进一步合成将产生具有更有效的抗结核活性的化合物。