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Zinc-oxaprozin compounds: Synthesis, structure and biological activity.
Journal of Inorganic Biochemistry ( IF 3.8 ) Pub Date : 2019-03-21 , DOI: 10.1016/j.jinorgbio.2019.03.016
Marialena Lazou 1 , Antonios G Hatzidimitriou 1 , Athanasios N Papadopoulos 2 , George Psomas 1
Affiliation  

Four novel zinc complexes, namely [Zn(oxa)2(MeOH)4] (1), [Zn(oxa)2(H2O)(bipy)]·MeOH·2.5H2O (2·MeOH·2.5H2O), [Zn(oxa)2(bipyam)]·1.25MeOH (3·1.25MeOH) and [Zn(oxa)2(phen)] (4), with the non-steroidal anti-inflammatory drug oxaprozin (Hoxa) and a N,N′-donor heterocyclic ligand, such as 2,2′‑bipyridylamine (bipyam), 1,10‑phenanthroline (phen) or 2,2′‑bipyridine (bipy), were characterized with physicochemical techniques, various spectroscopies and single-crystal X-ray crystallography. In these coordination compounds, the oxaprozin ligands are coordinated to zinc ion in a monodentate or a bidentate chelating binding mode. The antioxidant activity of the complexes was evaluated via their ability to scavenge in vitro 1,1‑diphenyl‑2‑picrylhydrazyl, hydroxyl and 2,2′‑azinobis‑(3‑ethylbenzothiazoline‑6‑sulfonic acid) radicals. The complexes bind to calf-thymus DNA via intercalation as suggested via a series of studies employing UV–vis spectroscopy, DNA-viscosity measurements and competition with ethidium bromide. The complexes may bind to serum albumins tightly and reversibly in order to get transferred through the bloodstream.



中文翻译:

氧杂丙嗪锌化合物:合成,结构和生物活性。

四种新型锌配合物,即[Zn(oxa)2(MeOH)4 ](1),[Zn(oxa)2(H 2 O)(bipy)]·MeOH·2.5H 2 O(2 ·MeOH·2.5H 2 O),[Zn(oxa)2(联苯胺)]·1.25MeOH(3 ·1.25MeOH)和[Zn(oxa)2(phen)](4),以及非甾体抗炎药oxaprozin(Hoxa )和NN通过物理化学技术,各种分光光度法和单晶X表征了'供体杂环配体,例如2,2'-联吡啶胺(bipyam),1,10-菲咯啉(phen)或2,2'-联吡啶(bipy)射线晶体学。在这些配位化合物中,奥沙普嗪配体以单齿或双齿螯合结合方式与锌离子配位。通过其清除体外1,1-二苯基-2-吡啶甲基肼基,羟基和2,2'-叠氮基双(3-乙基苯并噻唑啉-6-磺酸)基团的能力来评估复合物的抗氧化活性。结合的小牛胸腺DNA的复合物通过插层的建议经由使用紫外可见光谱,DNA粘度测量以及与溴化乙锭竞争的一系列研究。该复合物可以紧密和可逆地与血清白蛋白结合,以便通过血流转移。

更新日期:2019-03-21
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