| Synthesis, Structure Characterization, and Cu^2＋ Recognition of 3-{ [3- （Phenylsulfonamido） benzoyl ] methylidene } -3,4- dihydroquinoxaline-2 （1H） -one |
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| 作者姓名： | LI Xue-mei ZENG Cheng-chu NIU Li-ting YAN Hong ZHENG Da-wei ZHONG Ru-gang |
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| 作者单位： | College of Life Science ＆ Bioengineering, Beijing University of Technology, Beijing 100022, P. R. China |
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| 基金项目： | 国家自然科学基金，Special Foundation for Beijing Municipal Intelligent，北京市自然科学基金 |
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| 摘 要： | IntroductionSubstituted diketo acid derivatives possess a varie-ty of biological properties, such as analgesic1—3], anti-bacterial4]as well as anti-inflammatory3]. Very re-cently, the results of random screening of millions ofcompounds have shown that…
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| 关 键 词： | 二酮酸 奎喔酮 X-射线晶体结构 Cu^2＋识别 结构表征 合成 |
| 文章编号： | 1005-9040（2006）-06-747-06 |
| 收稿时间： | 2005-11-16 |
Synthesis, Structure Characterization, and Cu Recognition of 3- {[3-(Phenylsulfonamido) benzoyl] methylidene} -3, 4-dihydroquinoxaline-2 (1H) -one |
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| LI Xue-mei ZENG Cheng-chu NIU Li-ting YAN Hong ZHENG Da-wei ZHONG Ru-gang.Synthesis, Structure Characterization, and Cu Recognition of 3- {[3-(Phenylsulfonamido) benzoyl] methylidene} -3, 4-dihydroquinoxaline-2 (1H) -one[J].Chemical Research in Chinese University,2006,22(6):747-752. |
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| Authors: | Xue-mei LI Cheng-chu ZENG Li-ting NIU Hong YAN Da-wei ZHENG Ru-gang ZHONG |
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| Institution: | aCollege of Life Science & Bioengineering, Beijing University of Technology, Beijing 100022, P. R. China |
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| Abstract: | Aryl diketo acid derivatives are one of the most promising HIV-1 integrase(IN) inhibitors. With a view to substitute the critical diketo acid pharmacophore with the diketo benzimidazole unit, the coupling reaction of compound 4 with o-phenylenediamine was carried out. However, the reaction product, compound 5, was confirmed to be 3-{3-(phenylsulfonamido)benzoyl]methylidene}-3,4-dihydroquinoxaline-2(1H)-one rather than the 2-benzimidazole derivative by using X-ray diffraction. Owing to its low solubility in water, the evaluation of the anti-HIV IN activity of the synthesized compound 5 could not be carried out. Consequently, the ion-binding properties of compound 5 in the absence of HIV-1 IN were investigated with UV-Vis spectroscopy in organic solvents. The results show that such a compound can selectively recognize Cu~ 2 . |
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| Keywords: | Diketo acid Quinoxalone derivative X-ray crystal structure Cu~ 2 recognition |
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