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合成、抗氧化活性评价及 2,4-二甲基苯甲酰腙的晶体结构。

Synthesis, evaluation of antioxidant activity and crystal structure of 2,4-dimethylbenzoylhydrazones.

机构信息

Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA, Puncak Alam Campus, Bandar Puncak Alam 42300, Selangor, Malaysia.

出版信息

Molecules. 2013 Sep 5;18(9):10912-29. doi: 10.3390/molecules180910912.

Abstract

2,4-Dimethylbenzoylhydrazones 1-30 were synthesized by condensation reactions of 2,4-dimethylbenzoylhydrazide with various aromatic aldehydes and characterized. The assigned structures of compounds 10, 15 and 22 were further supported by single-crystal X-ray diffraction data. The synthesized compounds were evaluated for their in vitro DPPH radical scavenging activity. They exerted varying degree of scavenging activity toward DPPH radical with IC₅₀ values between 25.6-190 µM. Compounds 1, 4, 2, 3, 7, and 6 have IC₅₀ values of 25.6, 28.1, 29.3, 29.8, 30.0 and 30.1 µM respectively, showing better activity than an n-propyl gallate standard (IC₅₀ value = 30.30 µM). For super oxide anion scavenging activity compounds 1, 2 and 3 with IC₅₀ values of 98.3, 102.6, and 105.6, respectively, also showed better activity than the n-propyl gallate standard (IC₅₀ value = 106.34 µM).

摘要

2,4-二甲基苯甲酰腙 1-30 通过 2,4-二甲基苯甲酰肼与各种芳香醛的缩合反应合成,并进行了表征。化合物 10、15 和 22 的指定结构通过单晶 X 射线衍射数据进一步得到支持。合成的化合物进行了体外 DPPH 自由基清除活性评估。它们对 DPPH 自由基表现出不同程度的清除活性,IC₅₀ 值在 25.6-190 µM 之间。化合物 1、4、2、3、7 和 6 的 IC₅₀ 值分别为 25.6、28.1、29.3、29.8、30.0 和 30.1 µM,显示出比正丙基没食子酸酯标准(IC₅₀ 值=30.30 µM)更好的活性。对于超氧阴离子清除活性,化合物 1、2 和 3 的 IC₅₀ 值分别为 98.3、102.6 和 105.6,也显示出比正丙基没食子酸酯标准(IC₅₀ 值=106.34 µM)更好的活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7922/6269687/c9a02a823f25/molecules-18-10912-g004.jpg

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