Synthesis, antibacterial and free radical scavenging activity of some newer N-((10-nitro-1H-indolo [1, 2-c]quinazolin-12-yl)methylene)benzenamines

European Pharmaceutical Journal Pub Date : 2020-01-01 DOI:10.2478/afpuc-2020-0002

A. Dixit, D. Pathak, G. Sharma

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引用次数: 4

Abstract

Abstract Present research is oriented on the synthesis of some novel 12-(N-arylmethaniminyl)indolo[1,2-c]quinazoline analogs (4b1–4b11) and their characterization by 1H NMR, 13C NMR, FTIR and mass spectrophotometry. Their free radical scavenging activity and antibacterial potential were also evaluated. Many derivatives have shown a marked free radical scavenging capacity in all the concentrations but specifically compounds 4b7, 4b8 and 4b11 have shown good antioxidant potential with an IC50 value of 25.18 μmol/L, 28.09 μmol/L & 44.22 μmol/L, respectively (DPPH method) and 39.46 μmol/L, 44.47 μmol/L & 35.61 μmol/L, respectively (H2O2 method). The antibacterial evaluation was carried out against B. subtilis and E. coli by agar well diffusion method and it revealed that all the compounds in the series were having marked antibacterial activity but compounds 4b9 and 4b11 have shown best antibacterial potential. Then, it was concluded that the derivatives which were containing substituted anilines (4-Nitro, 4-Fluoro, 4-Bromo & 4-Chloro-2-nitro) on the carbon attached on the 12th position of indoloquinazoline moiety were having marked potential as an antibacterial and free radical scavenger.

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新型N-（（10-硝基-1H-吲哚[1,2-c]喹唑啉-12-基）亚甲基）苯胺的合成、抗菌及清除自由基活性

摘要本研究的重点是合成一些新型的12-（N-芳基甲烷亚氨基）吲哚并[1，2-c]喹唑啉类似物（4b1–4b11），并用1H NMR、13C NMR、FTIR和质谱法对其进行表征。并对其清除自由基的活性和抗菌潜力进行了评价。许多衍生物在所有浓度下都表现出显著的自由基清除能力，但特别是化合物4b7、4b8和4b11表现出良好的抗氧化潜力，IC50值分别为25.18μmol/L、28.09μmol/L和44.22μmol/L（DPPH法）和39.46μmol/L、44.47μmol/L和35.61μmol/L（H2O2法）。通过琼脂扩散法对枯草芽孢杆菌和大肠杆菌进行了抗菌评价，结果表明，该系列中的所有化合物都具有显著的抗菌活性，但化合物4b9和4b11显示出最佳的抗菌潜力。结果表明，在吲哚醌唑啉部分第12位的碳上含有取代苯胺（4-硝基、4-氟、4-溴和4-氯-2-硝基）的衍生物具有显著的抗菌和自由基清除剂潜力。

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来源期刊

European Pharmaceutical Journal Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)

CiteScore

0.60

自引率

0.00%

发文量

期刊介绍： European Pharmaceutical Journal publishes only original articles not previously published and articles that are not being considered or have not been submitted for publication elsewhere. If parts of the results have been published as conference abstract or elsewhere, it should be stated in references. The ethical standards of the Helsinki-Tokio Declaration should be kept. This should be mentioned in the Methods of manuscript. Reviews are published only on request. Authors, whose submitted research work was performed with the support of a company, should indicate this in Conflict of Interest.