Synthesis,Crystal Structure and Antitumor Activity of Mixed Ligand Coordination Compound of Copper with Norfloxacin and 1,10-Phen,[Cu(NFLX)(phen)(H_2O)] NO_3·3H_2O

Fluoroquinolones are the widely used antibiotics for treating of numerous diseases1-4. Norfloxacin(1-ethyl-6-fluoro-4-oxo-7-(1-piperazinyl)-1,4dihydroquinoline-3-carboxylicacid, NFLX) is a typical member of this family and its metal coordination compounds have also received much more attention5-11. Apart from the synthesis and physicochemical properties of the coordination compounds, their antibacterial properties were also tested7-13, but there was scare report on antitumor properties of th…     

诺氟沙星在胶束溶液中的荧光光谱特性及其应用

诺氟沙星在pH值为2.1的酒石酸-酒石酸钠缓冲溶液中具有较强的荧光,十二烷基磺酸钠(SDS)胶束溶液对诺氟沙星的荧光有增敏作用,线性范围为0.069 3~0.693 0μg/mL,回归方程为F=66.89c 0.149 4,相关系数为0.999 4,检出限为0.010 3μg/mL。用该法测定滴眼液和胶囊中诺氟沙星的含量,相对标准偏差为0.10%~0.93%,回收率为90.91%~108.5%。     

Digitally enhanced thin layer chromatography for simultaneous determination of norfloxacin and tinidazole with the aid of Taguchi orthogonal array and desirability function approach: Greenness assessment by analytical Eco‐Scale

In this study, an eco‐friendly fast simple method was developed for simultaneous determination of norfloxacin and tinidazole based on thin‐layer chromatography and image‐processing analysis. The binary mixture was separated using reversed phase ‐ thin layer chromatography plates and 30% trifluoroacetic acid only as mobile phase. Mobile phase composition was optimized using Taguchi orthogonal array and Derringer's desirability function. The plates were viewed under UV lamp and photographed by iPhone camera followed by image processing with Fiji software using integrated density as the measured response. As decreasing illumination increases the sensitivity of the method, this method was applied on two different ranges for each drug. The first one was 0.6–6.0 and 0.9–9.0 µg/spot for norfloxacin and tinidazole, respectively measured on the original image with normal illumination. The second one was measured after decreasing the illumination of the captured images at 0.06–0.60 and 0.09–0.90 µg/spot for norfloxacin and tinidazole, respectively. The proposed method was successfully applied for the determination of both drugs in tablets dosage form without interference from the commonly encountered excipients. Analytical Eco‐Scale was used to evaluate the greenness profile of the proposed method and it was found to be excellent green analytical method.     

Co(II), Mn(II) and Cu(II) complexes of fluoroquinolones: Synthesis, spectroscopical studies and biological evaluation against Trypanosoma cruzi

[MnCl₂(NOR)(H₂O)₂] (1), [MnCl₂(SPAR)(H₂O)₂] (2), [CoCl₂(NOR)(H₂O)₂] (3) [CoCl₂(SPAR)(H₂O)₂] (4), [CuCl₂(phen)(NOR)] (5) and [CuCl₂(phen)(SPAR)] (6) complexes with norfloxacin (NOR) and sparfloxacin (SPAR) were obtained from MnCl₂·4H₂O, CoCl₂·4H₂O and CuCl₂(phen). In all cases the NOR and SPAR coordinate in the neutral zwitterionic form. The electron paramagnetic resonance spectra of the Cu(II) complexes (5) and (6) in aqueous and DMSO solutions indicate mixture of mononuclear and binuclear complex. Complexes (1-6), together with the corresponding ligands were evaluated for their in vitro trypanocidal effect, against both bloodstream trypomastigotes and intracellular forms of Trypanosoma cruzi. SPAR and NOR were poorly effective upon T. cruzi, complexes (3) and (4) were active against intracellular forms of the parasite. The complexes (5) and (6) displayed a higher activity upon both bloodstream and intracellular forms. The potency of fluoroquinolones, specially those coordinated to Cu(II)-phen justify further trypanocidal screening assays with this compounds in vitro as well as upon experimental models of T. cruzi infection.     

电子受体与诺氟沙星的电荷转移反应

本文研究了电子受体对苯醌、２，３－二氰－５，６－二氯－１，４－对苯醌、四氯对苯醌和四溴对苯酯与诺氟沙星［１－乙基－６氟－１，４－二氢－１，４－二氢－４－氧人－７－（１－哌嗪基）喹啉－３－羧酸］电子给体之间的荷移反应。     

Fluoroquinolones’ Biological Activities against Laboratory Microbes and Cancer Cell Lines

Development of novel derivatives to rein in and fight bacteria have never been more demanding, as microbial resistance strains are alarmingly increasing. A multitude of new fluoroquinolones derivatives with an improved spectrum of activity and/or enhanced pharmacokinetics parameters have been widely explored. Reporting novel antimicrobial agents entails comparing their potential activity to their parent drugs; hence, parent fluoroquinolones have been used in research as positive controls. Given that these fluoroquinolones possess variable activities according to their generation, it is necessary to include parent compounds and market available antibiotics of the same class when investigating antimicrobial activity. Herein, we provide a detailed guide on the in vitro biological activity of fluoroquinolones based on experimental results published in the last years. This work permits researchers to compare and analyze potential fluoroquinolones as positive control agents and to evaluate changes occurring in their activities. More importantly, the selection of fluoroquinolones as positive controls by medicinal chemists when investigating novel FQs analogs must be correlated to the laboratory pathogen inquest for reliable results.     

高精度散射光度滴定法测定诺氟沙星的含量

用四苯硼钠标准溶液作滴定剂,采用高精度散射光度滴定法测定了诺氟沙星的含量,并将测定结果与非水滴定法、非水电位滴定法和高效液相色谱法的测定结果进行比较。结果表明：用本方法测定诺氟沙星的含量具有较高的准确度、精密度和良好的线性,且不受其降解产物的干扰。     

铁络合光度法测定氧氟沙星和诺氟沙星含量

研究了氧氟沙星、诺氟沙星与Fe(III)在室温下的络合反应.在酸性介质中,氧氟沙星、诺氟沙星与Fe(III)形成的黄色配合物最大吸收波长为436nm;氧氟沙星和诺氟沙星的浓度分别在2.24~192mg/L和8.0~248mg/L范围内与体系的吸光度呈良好的线性关系,其线性回归方程分别为:A=0.009 06+0.005 7 c(c,mg/L;r=0.999 3;氧氟沙星)和A=0.001 23+0.003 04 c(c,mg/L;r=0.999 8;诺氟沙星),方法的检出限分别为0.41和0.76mg/L.对浓度均为64.0mg/L的氧氟沙星和诺氟沙星平行测定11次,其相对标准偏差分别为0.6%和0.8%.应用拟定的方法对氧氟沙星和诺氟沙星药物制剂中主成分的含量进行了测定,回收率在99.7%~104.7%范围内.     

由氟哌酸构筑的铜(Ⅱ)配合物的合成、结构和抑菌性能（英文）

通过水热法合成了2种铜配合物[Cu2(HNOR)2Cl]n(1)和[Cu2Cl3]·H3NOR·H2O(2)(H2NOR=氟哌酸),并对其结构进行了X射线单晶衍射测定。结果表明,虽然反应物相同,但在酸度和碱度条件下分别生成具有不同结构的配合物。通过氢键和π-π相互作用,2种配合物形成了稳定的二维结构。同时,选择大肠杆菌和金黄色葡萄球菌作为革兰氏阳性和革兰氏阴性进行了抑菌活性实验。抑菌活性表明,2种配合物对大肠杆菌和金黄色葡萄球菌都有很好的抑制作用。     

诺氟沙星-DNA复合物的分子动力学模拟

采用分子模建的方法构建了诺氟沙星-DNA复合物的初始结构, 通过2 ns的分子动力学(MD)模拟研究表明: 诺氟沙星能够和双螺旋d[ATATCGATAT]₂形成稳定的复合物, 药物分子可紧密结合在DNA的小沟区域, 并且能够与DNA的鸟嘌呤碱基形成两个稳定的氢键. 在分子水平上提供了诺氟沙星直接与双螺旋DNA相互作用的结构及复合物的动态变化情况.