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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >One-pot microwave assisted synthesis under green chemistry conditions, antioxidant screening, and cytotoxicity assessments of benzimidazole Schiff bases and pyrimido(1,2-a)benzimidazol-3(4H)-ones.
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One-pot microwave assisted synthesis under green chemistry conditions, antioxidant screening, and cytotoxicity assessments of benzimidazole Schiff bases and pyrimido(1,2-a)benzimidazol-3(4H)-ones.

机译：在绿色化学条件下，一锅微波辅助合成，抗氧化剂筛选以及苯并咪唑席夫碱和嘧啶基（1,2-a）苯并咪唑-3（4H）-一的细胞毒性评估。

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摘要

The synthesis of a number of benzimidazole Schiff bases 3 and 3-oxo-pyrimido[1,2-a]benzimidazoles 4 in excellent yields by a one-step sequence from the reaction of 2-aminobenzimidazole under green chemistry conditions is described. Structural assignments of the new compounds as well as complete assignment of (1)H and (13)C NMR signals have been unambiguously achieved based on the analysis of their (1)H and (13)C NMR (1D and 2D), IR, MS and elemental analysis data. To the synthesized Schiff bases the E-configuration was assigned on the basis of comparison of experimental and calculated (DFT) (13)C NMR chemical shifts. Compounds 3 and 4 were evaluated as inhibitors of lipoxygenase (LOX) and of lipid peroxidation (LPO). All the tested derivatives showed inhibition of lipid peroxidation, whereas most of them were found to have higher activation than the reference compound trolox; The Schiff bases 3e, 3h, and 3i, and the pyrimidobenzimidazoles 4a, 4e and 4f were found to be the most potent. The most potent LOX inhibitor within the subset of Schiff bases was found compound 3i, followed by 3f, whereas compounds 4a and 4g were found the most potent of the 3-oxo-pyrimido[1,2-a]benzimidazole group. Moreover, some cytotoxicity assessments were undertaken, whereupon it was found that Schiff base 3i and pyrimidobenzimidazoles 4e and 4f did not exhibit cytotoxicity at similar concentrations resembling thus the inhibitory activity of lipid peroxidation. The most cytotoxic Schiff base and pyrimidobenzimidazole were found to be 3d and 4c, respectively.
机译：描述了一种由2-氨基苯并咪唑在绿色化学条件下的一步反应，以优异的产率合成了许多苯并咪唑席夫碱3和3-氧代-嘧啶并[1,2-a]苯并咪唑4。根据新化合物的（1）H和（13）C NMR（1D和2D），IR的分析，已明确实现了新化合物的结构分配以及（1）H和（13）C NMR信号的完整分配，MS和元素分析数据。在比较实验值和计算值（DFT）（13）C NMR化学位移的基础上，将E-构型分配给合成的Schiff碱。评价化合物3和4作为脂加氧酶（LOX）和脂质过氧化作用（LPO）的抑制剂。所有测试的衍生物均显示出对脂质过氧化的抑制作用，而发现大多数衍生物的活性均高于参比化合物trolox。发现席夫碱3e，3h和3i以及嘧啶基苯并咪唑4a，4e和4f最有效。在席夫碱子集中最有效的LOX抑制剂是化合物3i，然后是3f，而化合物4a和4g被发现是3-氧代嘧啶并[1,2-a]苯并咪唑基团中最有效的。此外，进行了一些细胞毒性评估，结果发现席夫碱3i和嘧啶基苯并咪唑4e和4f在相似的浓度下没有表现出细胞毒性，因此类似于脂质过氧化的抑制活性。发现最具细胞毒性的席夫碱和嘧啶苯并咪唑分别为3d和4c。

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