Design, synthesis and antifibrotic activities of carbohydrate-modified 1-(substituted aryl)-5-trifluoromethyl-2(1H) pyridones

Pirfenidone, a pyridone compound, is an effective and novel antifibrotic agent. In this article, we describe the design, synthesis and activity evaluation of novel antifibrotic agents, 1-(substituted aryl)-5-trifluoromethyl-2(1H) pyridones modified with carbohydrate. Most of the title compounds exhibited comparable or better inhibitory activity than fluorofenidone. Notably, compound 19a demonstrated the highest cell-based inhibitory activity against NIH 3T3 (IC(50) = 0.17 mM).     

(2-羧基苯氧基)苯-1,2-二羧酸构筑的镧系配合物对苯甲醛和阳离子的荧光传感

采用水热法合成了5个稀土配合物[Sm₂(bdbc)₂(phen)₄](1)和[Ln(bdbc)(phen)(H₂O)][Ln=Eu(2), Gd(3), Tb(4), Dy(5), bdbc=(2-羧基苯氧基)苯-1,2-二羧酸根, phen=1,10-邻菲啰啉]. 配合物1是双核分子, 通过氢键和C—H…π作用进一步构筑成一维超分子结构; 配合物2~5是同构的一维双螺旋结构, 通过氢键和C—H…π作用进一步构筑成三维超分子结构. 配合物1, 2, 4和5呈现了Sm³⁺, Eu³⁺, Tb³⁺和Dy³⁺离子的特征发射, 分别对应于Sm³⁺离子的⁴G_5/2→⁶H_J/2(J=5, 7, 9)、 Eu³⁺离子的⁵D₀→⁷F_J(J=1—4)、 Tb³⁺离子的⁵D₄→⁷F_J(J=6, 5, 4, 3)和Dy³⁺离子的⁴F_5/2→⁶H_J/2(J=15, 13)跃迁. 对配合物4的荧光性质进行了表征, 结果表明, 配合物4可用作荧光探针以检测阳离子和苯甲醛.     

燃烧法测定氧化矿捕收剂吸附量

虽然有很多现代测试技术可以用来测定脂肪酸类捕收剂在氧化矿表面的吸附量,但灵敏、方便和实用的方法并不多.燃烧法测定脂肪酸类捕收剂在氧化矿表面的吸附量具有速度快,设备简单的优点,具有很强的实用性,非常适合于氧化矿浮选捕收剂的试验研究.主要对燃烧法中差热分析法、载流燃烧法和顶空气相红外分析法的发展现状与应用进行了评述.     

Z,E型—α—氯代桂皮酰胺类化合物的合成与抗惊活性的研究

由E,Z型-α-氯代桂皮酸经酰氯、胺解及层析分离制得10对Z,E型异构体。其中Z型-对溴-α-氯代桂皮酰另丁胺的抗惊作用(MES)较强。药理实验表明这些异构体的构型、酰胺氮上的取代基对其生物活性有重大影响。     

Design, synthesis and anti-fibrosis activity study of N₁-substituted phenylhydroquinolinone derivatives

Pirfenidone (5-methyl-1-phenyl-2(1H)-pyridone, PFD) is a small-molecule compound acting on multiple targets involved in pathological fibrogenesis and is effective to increase the survival of patients with fibrosis, such as idiopathic pulmonary fibrosis. However, PFD is not active enough, requiring a high daily dose. In this study, to keep the multiple target profiles, N?-substituted phenylhydroquinolinone derivatives, which retain the 1-phenyl-2(1H)-pyridone scaffold were designed and synthesized. The preliminary anti-fibrosis activities for all target compounds were evaluated on a NIH3T3 fibroblast cell line using MTT assay methods. Most compounds showed significant inhibition on NIH3T3 cell proliferation with a IC?? range of 0.09-26 mM, among which 5-hydroxy-1-(4'-bromophenyl)-5,6,7,8-tetrahydroquinolin-2(1H)-one (6j) displayed 13 times higher potency (IC?? = 0.3 mM) than that of AKF-PD (IC?? = 4.2 mM). These results suggest that N?-substituted phenylhydroquinolinone is a promising scaffold which can be applied for further investigation and for developing novel anti-fibrosis agents.     

我国稀土浮选药剂研究进展

简要介绍了自60年代以来，我国研制和应用的含氮浮选药剂，稀土浮选含磷药剂，稀土羧酸类浮选剂及混合用药等几类主要稀土浮选药剂及其浮选性能和作用机理，阐述了稀土浮选体系的药剂交互作用规律。并探讨稀土浮选药剂研究的发展方向，稀土浮选药剂的研究正在向3个方向发展：一是研制新型高效浮选剂；二是对现有的药剂进行混合使用的研究，三是对稀土浮选体系中药剂的交互作用进行研究。     

Simultaneous LC–UV Determination of 5-Methyl-1-(3-fluorophenyl)-2-(1H)- pyridone and Its Two Metabolites in Rat Plasma

A simple, rapid, and reproducible isocratic reverse-phase HPLC method was developed to simultaneously determine AKF-PD and its two oxidized metabolites in rat plasma. 5-Carboxyl-1-phenyl-2-(1H)-pyridone and phenacetin were used as internal standards to ensure the precision and accuracy of the method. The analytes were separated on a C₁₈ reversed-phase column with methanol—phosphate buffer (20 mM, pH 2.5) as mobile phase. The limits of detection for AKF-PD and its two oxidized metabolites was 0.1 μg mL⁻¹. The method is applicable for the pharmacokinetic studies of AKF-PD and its metabolites in rats.

     

定容-氧气循环燃烧法测定捕收剂的吸附量

研究了一种定容-氧气循环燃烧法测定捕收剂吸附量的方法,并与传统的溶剂萃取-分光光度法进行了比较。实验表明,定容-氧气循环燃烧法较溶剂萃取-分光光度法测定油酸钠在磷矿石表面的吸附量更简便、准确。     

Simultaneous LC–UV Determination of 5-Methyl-1-(3-fluorophenyl)-2-(1H)- pyridone and Its Two Metabolites in Rat Plasma

A simple, rapid, and reproducible isocratic reverse-phase HPLC method was developed to simultaneously determine AKF-PD and its two oxidized metabolites in rat plasma. 5-Carboxyl-1-phenyl-2-(1H)-pyridone and phenacetin were used as internal standards to ensure the precision and accuracy of the method. The analytes were separated on a C₁₈ reversed-phase column with methanol—phosphate buffer (20 mM, pH 2.5) as mobile phase. The limits of detection for AKF-PD and its two oxidized metabolites was 0.1 μg mL^?1. The method is applicable for the pharmacokinetic studies of AKF-PD and its metabolites in rats.     

A chemically unlocked binary molecular switch

A highly luminescent and sensitive terbium complex of a ligand comprising of a phthalimide group appended to a DO3A moiety is an active pH sensor that is conditional on its previous pH.