...
首页> 外文期刊>RSC Advances >DNA interaction, cytotoxicity, antibacterial and antituberculosis activity of oxovanadium(IV) complexes derived from fluoroquinolones and 4-hydroxy-5-((4-hydroxyphenyl)diazenyl)thiazole-2(3H)-thione
【24h】

DNA interaction, cytotoxicity, antibacterial and antituberculosis activity of oxovanadium(IV) complexes derived from fluoroquinolones and 4-hydroxy-5-((4-hydroxyphenyl)diazenyl)thiazole-2(3H)-thione

机译:氟喹诺酮和4-羟基-5-((4-羟基苯基)二氮烯基)噻唑-2(3H)-硫酮衍生的氧钒(IV)配合物的DNA相互作用,细胞毒性,抗菌和抗结核活性

获取原文
获取原文并翻译 | 示例

摘要

Oxovanadium complexes (5a-5g) with fluoroquinolone ligands and azodye rhodanine (4-hydroxy-5-((4-hydroxyphenyl)diazenyl)thiazole-2(3H)-thione) were synthesized and the effect of different groups was studied, which displayed various biological and medicinal activities. The newly formed compounds were characterized using ESI-MS, UV-vis, IR, ESR spectroscopy, elemental analysis and molar electric conductivity. The in vitro antibacterial activity of the complexes against three Gram negative and two Gram positive microorganisms was studied and compared to the activity of free ligand and it shows considerable results. The minimum inhibitory concentration (MIC) of the compounds against Mycobacterium tuberculosis was determined and among all the complexes, 5c and 5d showed potency. The in vitro cytotoxicity of the complexes was determined with a brine shrimp bioassay and the LD50 obtained is in the range of 4-12 mu g mL(-1). The DNA binding activity was studied using UV-vis titration and viscosity measurements, and 5c has the highest binding constant value (6.91 x 10(5) M-1). DNA nuclease activity was studied using the agarose gel electrophoresis method and the compounds show 70-80% cleavage.
机译:合成了具有氟喹诺酮配体和偶氮染料若丹宁(4-羟基-5-((4-羟基苯基)二氮烯基)噻唑-2(3H)-硫酮)的氧钒络合物(5a-5g),并研究了不同基团的作用,表明各种生物和医学活动。使用ESI-MS,UV-vis,IR,ESR光谱,元素分析和摩尔电导率对新形成的化合物进行了表征。研究了该复合物对三种革兰氏阴性和两种革兰氏阳性微生物的体外抗菌活性,并将其与游离配体的活性进行了比较,并显示出可观的结果。确定了化合物对结核分枝杆菌的最小抑制浓度(MIC),并且在所有复合物中,5c和5d显示出效力。用盐水虾生物测定法测定了复合物的体外细胞毒性,得到的LD50在4-12μg mL(-1)范围内。使用UV-vis滴定法和粘度测量研究了DNA结合活性,并且5c具有最高的结合常数(6.91 x 10(5)M-1)。使用琼脂糖凝胶电泳方法研究了DNA核酸酶的活性,该化合物显示出70-80%的裂解。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号