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Synthesis of New Cyanopyridine Scaffolds and Their Biological Broadcast.
Current Organic Synthesis ( IF 1.7 ) Pub Date : 2020-10-31 , DOI: 10.2174/1570179417666200628020602
Nabil A Alhakamy 1, 2 , Ahmad O Noor 3 , Khaled M Hosny 1 , Jenny Jeehan Nasr 4 , Moustafa M G Fouda 5 , Tawfik A Khattab 6 , Hatem E Gaffer 6
Affiliation  

Background: 3-Cyanopyridine analogues are significant moieties with a variety of biological effects such as antioxidant, antimicrobial, anti-inflammatory and cytotoxic agents. In addition, they could be applied in the treatment of several diseases.

Objective: The study conducted cyclo-addition of 3a-e derivatives with malononitrile to yield the corresponding 6-(4-((3-cyano-pyridinyl) amino) phenyl)-4-phenylnicotinonitriles 4a-e.

Materials and Methods: Physical and spectral analyses were performed to demonstrate the proper structures of all incorporated analogues. The in vitro antimicrobial activity of the preps derivatives was investigated by testing them with a panel of pathogenic strains of bacteria and fungi. The anti-tuberculosis activity was observed against the Mycobacterium tuberculosis H37Rv strain. When examining cytotoxic agents for four different cell lines, researchers found that their activity was persuasive compared with that of standard antibiotics. In addition, the antioxidant activity of the synthesized analogues was evaluated using the DPPH method.

Results and Discussions: The synthesized analogues were examined to determine their activity against the M. tuberculosis H37Rv strain. Derivatives 2c, 2e, 3d and 3e had good inhibition. Further screening was done for the highest potency against M. tuberculosis to determine the MICs. The antioxidant efficacy was evaluated via the DPPH technique matched with vitamin C as a positive control. The prospective results showed that the derivatives did not display scavenging efficacies in comparison with the standard.

Conclusion: Some synthesized derivatives displayed good potency against bacterial activity and M. Tuberculosis. However, the antioxidant performance of these derivatives did not display scavenging efficacies compared to vitamin C. The cytotoxic activity of the synthesized derivatives was examined against various cell lines to display good cytotoxic activity in the order 4a-e > 2a-e > 3a-b.



中文翻译:

新型氰基吡啶支架的合成及其生物广播。

背景:3-氰基吡啶类似物是具有多种生物学效应的重要部分,例如抗氧化剂、抗菌剂、抗炎剂和细胞毒剂。此外,它们还可用于治疗多种疾病。

目的:该研究进行了 3a-e 衍生物与丙二腈的环加成反应,得到相应的 6-(4-((3-cyano-pyridinyl) 氨基) 苯基)-4-苯基烟腈 4a-e。

材料和方法:进行物理和光谱分析以证明所有掺入的类似物的正确结构。通过用一组细菌和真菌的致病菌株对其进行测试,研究了制备衍生物的体外抗微生物活性。观察到针对结核分枝杆菌 H37Rv 菌株的抗结核活性。在检查四种不同细胞系的细胞毒剂时,研究人员发现与标准抗生素相比,它们的活性具有说服力。此外,合成类似物的抗氧化活性使用 DPPH 方法进行评估。

结果和讨论: 检查合成的类似物以确定它们对结核分枝杆菌 H37Rv 菌株的活性。衍生物2c、2e、3d和3e具有良好的抑制作用。对针对结核分枝杆菌的最高效力进行了进一步筛选,以确定 MIC。通过DPPH技术与作为阳性对照的维生素C相匹配来评估抗氧化功效。前瞻性结果表明,与标准品相比,衍生物没有表现出清除功效。

结论:一些合成的衍生物对细菌活性和结核分枝杆菌表现出良好的效力。然而,与维生素 C 相比,这些衍生物的抗氧化性能没有表现出清除功效。 针对各种细胞系检查合成衍生物的细胞毒活性,以 4a-e > 2a-e > 3a-b 的顺序显示出良好的细胞毒活性.

更新日期:2020-10-30
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