叶绿素及其Cu、Zn衍生物的伪装性能研究

研究了类叶绿素活性颜料在伪装应用中的光谱性能及光稳定性问题。从绿色植被的色素着手,分析了叶绿素的性质及影响其降解的原因,用Cu2+、Zn2+金属离子替代天然叶绿素中的Mg2+,制备了叶绿素衍生物,并通过光谱特性和光稳定性对叶绿素衍生物的特性进行了比较分析。研究结果表明,从光谱性能和稳定性两方面综合考虑,Cu叶绿素更适合作为叶绿素修饰目标来提高颜料的稳定性,从而为新型光学伪装涂料的制备提供材料基础。     

Synthesis and characterization of coumarin thiazole derivative 2-(2-amino-1,3-thiazol-4-yl)-3H-benzo[f]chromen-3-one with anti-microbial activity and its potential application in antimicrobial polyurethane coating

Coumarin, thiazole and their respective derivative products are some of the oldest and most commonly known class of nitrogen and sulphur containing compounds. In recent years there has been considerable interest in this coumarin–thiazole derivatives, which have been reported to exhibit significant biological activity and are widely used as pharmaceuticals. They are capable of imparting anti-microbial activity properties when incorporated into polymers and polymer composites. In this research, coumarin–thiazole derivative 2-(2-amino-1,3-thiazol-4-yl)-3H benzo[f]chromen-3-one (compound III), was prepared and its structure was confirmed by means of its spectra data. It was also screened for its anti-microbial activity against eight different micro-organisms when physically incorporated into a polyurethane varnish formula. Experimental coatings were manufactured on a laboratory scale and applied by means of a brush on both glass and steel panels. The results of the biological activity indicated that the polyurethane varnishes containing the 2-(2-amino-1,3-thiazol-4-yl)-3H-benzo[f]chromen-3-one (compound III) derivative, exhibit a very good antimicrobial effect. The molecular modeling study revealed that it is biologically safe, it is active and it fulfills Lipinski's rule of five. The physical and mechanical resistances of the polyurethane varnish formulations were also studied to evaluate any drawbacks associated with the addition of the derivative. The studies indicate that the physical incorporation of compound III actually enhances slightly both the physical and mechanical properties.     

Direct Construction of the 9H‐Pyrrolo[1,2‐a]azepin‐9‐amine Skeleton via [4+3] Annulation of Alkyl 2‐Aroyl‐1‐chlorocyclo‐ propanecarboxylates

A direct diastereoselective synthesis approach of important 9H‐pyrrolo[1,2‐a]azepin‐9‐amines was established via base‐promoted [4+3] annulation between donor–acceptor reagents derived from 1H‐pyrrole‐2‐carbaldehydes and alkyl 2‐aroyl‐1‐chlorocyclopropanecarboxylates. This transition metal‐free domino reaction proceeded quickly under mild basic conditions, affording potentially bioactive azepine derivatives in moderate to high yields with high diastereoselectivities (up to >20:1).

     

A process for the complete fractionation of baker's yeast

A process for the preparation of yeast-derived food additives was developed. The four products obtained, yeast protein concentrate (YPC), cell-wall protein (CWP), semi-pure glucomannan (SPG) and yeast extract, compared well with similar products, present in the current market, with respect to functional properties. YPC and CWP exhibited improved water-holding and oil-binding properties over those of soy-protein isolate (SPI). The emulsifying capacity was very close to that observed in commercial samples. A one-step alkaline extraction enhanced the functional properties of primary yeast glycan to match traditional food hydrocolloid sources. SPG showed oil-binding properties significantly greater than commercial glucomannan.     

The Effect of Fullerenol C60(OH)36 on the Antioxidant Defense System in Erythrocytes

Background: Fullerenols (water-soluble derivatives of fullerenes), such as C₆₀(OH)₃₆, are biocompatible molecules with a high ability to scavenge reactive oxygen species (ROS), but the mechanism of their antioxidant action and cooperation with endogenous redox machinery remains unrecognized. Fullerenols rapidly distribute through blood cells; therefore, we investigated the effect of C₆₀(OH)₃₆ on the antioxidant defense system in erythrocytes during their prolonged incubation. Methods: Human erythrocytes were treated with fullerenol at concentrations of 50–150 µg/mL, incubated for 3 and 48 h at 37 °C, and then hemolyzed. The level of oxidative stress was determined by examining the level of thiol groups, the activity of antioxidant enzymes (catalase, glutathione peroxidase, glutathione reductase, and glutathione transferase), and by measuring erythrocyte microviscosity. Results: The level of thiol groups in stored erythrocytes decreased; however, in the presence of higher concentrations of C₆₀(OH)₃₆ (100 and 150 µg/mL), the level of -SH groups increased compared to the control. Extending the incubation to 48 h caused a decrease in antioxidant enzyme activity, but the addition of fullerenol, especially at higher concentrations (100–150 µg/mL), increased its activity. We observed that C₆₀(OH)₃₆ had no effect on the microviscosity of the interior of the erythrocytes. Conclusions: In conclusion, our results indicated that water-soluble C₆₀(OH)₃₆ has antioxidant potential and efficiently supports the enzymatic antioxidant system within the cell. These effects are probably related to the direct interaction of C₆₀(OH)₃₆ with the enzyme that causes its structural changes.     

4-(2-噻吩基)苯乙酸及其衍生物的合成

采用新方法设计并合成了4-(2-噻吩基)苯乙酸及其衍生物。通过对各步反应的研究,找到了最佳的反应条件和4-(2-噻吩基)苯乙酸及其衍生物的分离和纯化方法。并对这些化合物的结构用元素分析I、R1、H NMR进行了确证。并对其潜在的应用价值进行了探讨。     

N,N′,N″-三(异丙基)-1,4,7-三氮杂环壬烷的合成改进

在无水碳酸钾存在下,以1,4,7-三氮杂环壬烷和2-溴丙烷为原料合成了标题化合物,与文献方法相比,产物处理简单,产率高达99%。     

径基函数-自适应偏最小二乘回归方法辅助含硫苯衍生物分子设计

针对药物构效关系呈非线性的特征,提出一种径基函数(radial basis function,RBF)-自适应偏最小二乘回归(adaptive partial least squares regression,APLSR)相结合的建模方法。该组合方法应用RBF实现自变量非线性变换,应用APLSR方法消除非线性变换后输出变量间存在的复共线性,并以模型的预报能力为目标,自适应地确定PLSR模型的最佳隐变量个数,从而获得预报性能良好的模型。本文将RBF-APLSR方法应用于含硫苯衍生物的定量构效关系建模,取得了令人满意的效果,其预报精度高于PLSR方法。     

平板颤振导数的参数弹性研究

提出了颤振导数的“参数弹性”概念;基于复模态理论,计算了平板颤振导数的平板宽度、质量、质量惯矩、竖弯频率、扭转频率和空气密度6种参数弹性;绘制了8个颤振导数的参数弹性曲线和诺模图,分析了各自特点,获得了无量纲参数对颤振导数参数弹性的影响规律。分析结果表明,新提出的参数弹性具有概念无量纲、简洁、直观、实用特点,为颤振导数参数分析提供了一种新的有效途径。     

Friction and wear characteristics of organic thiophosphoro derivatives — a critical appraisal

The friction- and wear-reducing characteristics of a number of oil soluble sulphurised and phosphosulphurised derivatives for automotive and industrial applications have been reviewed. A critical appraisal of the suggested causes and mechanism of friction reduction and antiwear characteristics has been made. A review of the investigations carried out so far indicates that the creation of in situ films of simple inorganic salts, such as molybdenum disulphide, iron sulphide or phosphates of low shear strength and lamellar structures, does not appear to be the primary cause of low friction and wear. The authors have, therefore, undertaken a programme to synthesise and study the chemistry and tribochemical reactions in relation to friction and wear characteristics of hydrocarbon-soluble thiophosphoro derivatives of alkyl phenol, alcohols and fatty esters, in order to establish relationships between the reactivity, chemical nature and crystal structure of films formed on rubbing surfaces, and antifriction and antiwear characteristics. Molybdenum salts of various phosphorothio derivatives of pentadecylphenol and lauryl oleate of specific structures have been synthesised, and the friction and wear properties of their blends in mineral oil base stock have been studied. It can be clearly inferred from the results that type of bonding between sulphur, phosphorus and molybdenum, and reactivity of these derivatives with rubbing surfaces, determine their friction-reducing and antiwear characteristics. Their reactivity with iron and the nature of films formed are under investigation.