新型 2,4-二硝基苯衍生物的合成与生物活性测定。
Synthesis and determination of some biological activities of novel 2,4-dinitrophenyl derivatives.
机构信息
Engineering and Natural Sciences Faculty, Food Engineering Department, Gumushane University, Gumushane, Turkey.
出版信息
Arch Pharm (Weinheim). 2015 Mar;348(3):214-20. doi: 10.1002/ardp.201400330. Epub 2015 Feb 2.
The antioxidant and radical scavenging activities of the synthesized compounds 3, 5, and 6 were determined by various in vitro assays such as 2,2-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid radical (ABTS(·+) ) scavenging, ferric ion (Fe(3+) ) reducing power and ferrous ion (Fe(2+) ) chelating activities. Moreover, these activities were compared to those of standard antioxidants such as butylated hydroxyanisole, butylated hydroxytoluene, and trolox. The results showed that the new compounds (3, 5, and 6) had potential antioxidant activity. Besides, inhibition of the two human cytosolic carbonic anhydrase (hCA, EC 4.2.1.1) isozymes I and II with some nitrobenzene compounds was investigated. Compounds 1-6 showed Ki values in the range of 4.88-193.4 µM and 5.295-54.75 µM for hCA I and hCA II, respectively.
合成的化合物 3、5 和 6 的抗氧化和自由基清除活性通过各种体外测定方法来确定，如 2,2-偶氮-双(3-乙基苯并噻唑啉-6-磺酸自由基（ABTS(·+)）清除、铁离子（Fe(3+)）还原能力和亚铁离子（Fe(2+)）螯合活性。此外，将这些活性与标准抗氧化剂如丁基羟基茴香醚、丁基羟基甲苯和 Trolox 进行了比较。结果表明，新化合物（3、5 和 6）具有潜在的抗氧化活性。此外，还研究了一些硝基苯化合物对两种人胞质碳酸酐酶（hCA，EC 4.2.1.1）同工酶 I 和 II 的抑制作用。化合物 1-6 对 hCA I 和 hCA II 的 Ki 值分别在 4.88-193.4 μM 和 5.295-54.75 μM 的范围内。
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