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新型吲哚衍生物的合成、抗氧化和 DNA 断裂活性。

Synthesis, antioxidant and DNA cleavage activities of novel indole derivatives.

机构信息

Central Research Lab, Department of Chemistry, Gulbarga University, Gulbarga, 585106 Karnataka, India.

出版信息

Eur J Med Chem. 2010 Sep;45(9):4074-8. doi: 10.1016/j.ejmech.2010.05.067. Epub 2010 Jun 9.

Abstract

A new series of novel indole derivatives containing barbitone moiety (5a-i) are synthesized by simple and efficient condensation of chalcones (3a-i) with barbituric acid (4). The synthesized compounds are screened for their antioxidant (free radical scavenging, total antioxidant capacity and ferric reducing antioxidant power) and DNA cleavage activities were evaluated. Among the synthesized compounds (5a), (5d) and (5g) exhibited excellent antioxidant activity and all the tested compounds in the series have exhibited promising DNA cleavage activities. The structures of the synthesized compounds are assigned on the basis of elemental analysis, IR, (1)H NMR, (13)C NMR and mass spectral data.

摘要

通过简单高效的查尔酮(3a-i)与巴比妥酸(4)缩合,合成了一系列新型含巴比妥部分的吲哚衍生物(5a-i)。对合成的化合物进行了抗氧化(自由基清除、总抗氧化能力和铁还原抗氧化能力)和 DNA 切割活性的筛选。在所合成的化合物中(5a)、(5d)和(5g)表现出优异的抗氧化活性,该系列中所有测试的化合物都表现出有希望的 DNA 切割活性。根据元素分析、IR、(1)H NMR、(13)C NMR 和质谱数据确定了合成化合物的结构。

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