Chandrasekhar Mandala, Syam Prasad Gandavaram, Venkataramaiah Chintha, Umapriya Kollu, Raju Chamarthi Naga, Seshaiah Kalluru, Rajendra Wudayagiri
Department of Chemistry, Sri Venkateswara University, Tirupati, India.
Departments of Zoology, Sri Venkateswara University, Tirupati, India.
J Recept Signal Transduct Res. 2020 Feb;40(1):34-41. doi: 10.1080/10799893.2019.1710848. Epub 2020 Jan 7.
Synthesis of a series of new urea and thiourea compounds have been accomplished by the reaction of 2,3-dihydro-1-inden-1-amine with various phenyl isocyanates and isothiocyanates. These compounds were evaluated for their antioxidant activity by using 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and nitric oxide (NO) radical scavenging assay methods including IC values. Some of the compounds exhibited potential activity in the two tested methods. Among the series of compounds, urea derivative linked with 4-bromo phenyl ring (), and thiourea derivatives bonded with phenyl ring (), 4-fluoro phenyl ring () and 4-nitro pheyl ring () were found to exhibit promising anti oxidant activity with low IC values. Where four of the title comounds exhibited higher bindig energies than the reference compound (Imatinib) in molecular docking studies with Aromatase. All the synthesized compounds were characterized by IR, H, C NMR and mass spectral data.
通过2,3 - 二氢 - 1 - 茚 - 1 - 胺与各种苯基异氰酸酯和异硫氰酸酯的反应,完成了一系列新的脲和硫脲化合物的合成。使用1,1 - 二苯基 - 2 - 苦基肼基(DPPH)自由基和一氧化氮(NO)自由基清除测定方法(包括IC值)对这些化合物的抗氧化活性进行了评估。一些化合物在两种测试方法中表现出潜在活性。在该系列化合物中,发现与4 - 溴苯环相连的脲衍生物()以及与苯环()、4 - 氟苯环()和4 - 硝基苯环()键合的硫脲衍生物表现出具有低IC值的有前景的抗氧化活性。其中,在与芳香酶的分子对接研究中,四种标题化合物表现出比参考化合物(伊马替尼)更高的结合能。所有合成的化合物均通过红外光谱、氢谱、碳谱和质谱数据进行了表征。