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Synthesis, admetSAR Predictions, DPPH Radical Scavenging Activity, and Potent Anti-mycobacterial Studies of Hydrazones of Substituted 4-(anilino methyl) benzohydrazides (Part 2)
Current Computer-Aided Drug Design ( IF 1.5 ) Pub Date : 2021-06-30 , DOI: 10.2174/1573409916666200615141047
Vijay J Desale 1 , Suraj N Mali 2 , Bapu R Thorat 1 , Ramesh S Yamgar 3
Affiliation  

Background: For the past several decades, the presence of tuberculosis (TB) is being remarked as the most common infectious disease leading to mortality.

Objective: Hydrazone containing azometine group (-NHN=CH-) compounds have been reported for a broad range of bioactivities such as antiplatelet, analgesic, anti-inflammatory, anticonvulsant, antidepressant, antimalarial, vasodilator, antiviral, and antimicrobial, etc.

Methods: For the synthesis of compounds (4a-4d) and (6a-6e), aromatic amines were treated with methyl terephthalaldehydate in methanol, giving Schiff’s bases, followed by reductive amination and further treatment with hydrazine hydrate gave acid hydrazides (4a-4d). These acid hydrazides were then treated with different aromatic aldehydes to yield hydrazones (6a-6d). All the synthesized compounds were subjected to FT-IR, NMR, and UV spectroscopic characterization.

Results: Compounds (4a-4d) and (6a-6e) were found to have highly potent activity against Mycobacteria tuberculosis (Vaccine strain, H37 RV strains): ATCC No- 27294 (MIC:1.6-6.25 μg/mL) than standard anti-TB drugs. The compounds exhibited good radical scavenging potentials(0- 69.2%), as checked from DPPH protocol. All compounds also demonstrated good in-silico ADMET results.

Conclusion: The current study revealed promising in vitro anti-tuberculosis and anti-oxidant profiles of hydrazide-hydrazone analogues.



中文翻译:

取代的 4-(苯胺基甲基)苯并酰肼的腙的合成、admetSAR 预测、DPPH 自由基清除活性和有效的抗分枝杆菌研究(第 2 部分)

背景:在过去的几十年中,结核病 (TB) 的存在被认为是导致死亡的最常见传染病。

目的:含氮唑汀基(-NHN=CH-)的腙类化合物具有广泛的生物活性,如抗血小板、镇痛、抗炎、抗惊厥、抗抑郁、抗疟疾、血管扩张剂、抗病毒和抗菌等。

方法:为了合成化合物(4a-4d)和(6a-6e),芳香胺在甲醇中用对苯二甲酸甲酯处理,得到席夫碱,然后还原胺化,再用水合肼处理得到酰肼(4a-4d) )。然后用不同的芳香醛处理这些酸酰肼以产生腙(6a-6d)。所有合成的化合物都进行了 FT-IR、NMR 和 UV 光谱表征。

结果:发现化合物(4a-4d)和(6a-6e)对结核分枝杆菌(疫苗株,H37 RV株)具有高效活性:ATCC No-27294(MIC:1.6-6.25 μg/mL)比标准抗- 结核病药物。从 DPPH 协议检查,化合物表现出良好的自由基清除潜力 (0-69.2%)。所有化合物也表现出良好的计算机 ADMET 结果。

结论:目前的研究揭示了酰肼-腙类似物的有希望的体外抗结核和抗氧化特性。

更新日期:2021-06-30
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