Synthesis and Insulin—sensitizing Activity of a Series of 2—Benzyl—1,3—dicarbonyl Derivatives

A series of 2-benzyl-1,3-dicabonyl derivatives was synthesized.Their insulin-sensitizing activity was evaluated in 3T3-L1 preadipocyte cells.Compounds3,26 and 27 were found to possess strong insulin-sensitizing activity in vitro and were selected for further hypoglycemic evaluation in vivo.     

烟酸对酸性硫酸盐体系铜电沉积的影响

对溶液A: 0.8 mol•L－1硫酸铜,0.6 mol•L－1硫酸,5.0×10－5 mol•L－1氯离子,1.0×10－4 mol•L－1聚乙二醇的溶液,溶液B:在溶液A中加入2.0×10－2 mol•L－1烟酸,pH为0.5,运用循环伏安和计时安培法研究玻碳电极上铜的电沉积行为.结果表明,铜的电沉积过程经历了晶核形成过程,其电结晶按瞬时成核和三维生长方式进行.烟酸的加入对铜的电沉积具有阻化作用,但不改变铜的电结晶机理.沉积层的X射线衍射表明Cu为面心立方结构,在烟酸存在下沉积层出现(220)高择优取向,这可能是烟酸在Cu(220)晶面上发生强烈吸附作用的结果.     

卟啉作为信号传递介质的紫外可见光谱研究

合成了6种氨基酸水杨醛席夫碱(Sal-AA)：Sal-Gly(甘氨酸)、Sal-Phe(苯丙氨酸)、Sal-Arg(精氨酸)、Sal-Tyr(酪氨酸)、Sal-Met(甲硫氨酸)、Sal-Glu(谷氨酸)及其金属铜配合物。并分别在2种不同介质(三氯甲烷和甲醇)中，与四苯基卟啉TPP进行反应，研究了其紫外可见光谱性质，讨论了卟啉作为人工信号转导体系的传递介质，与氨基酸水杨醛席夫碱铜配合物的反应中，实现信号分子铜离子进一步传递的可能性以及溶剂对该信号传递的影响。结果表明，在三氯甲烷为溶剂时，除了Sal-Met的铜配合物之外，其余均能被TPP夺取而形成Metal TPP。而在以甲醇为溶剂时，只有Sal-Gly的铜配合物能被TPP所夺取。     

Reduction of 4-nitrophenol catalyzed by nitroreductase

The reduction of 4-nitrophenol catalyzed by nitroreductase in the presence of NADH was investigated in this paper.4-Amino- phenol and 4-bydroxylamino-phenol were found in the reductive products.The relationship between reaction time and the reductive ratio were studied.The similar reducing ratios of 4-nitrophenol were obtained under aerobic and anaerobic conditions.The results indicated that an oxygen-insensitive reaction was proceeded in the reduction of 4-nitrophenol and nitroreductase was an oxygen- insensitive enzyme.The reductive products of 4-nitrophenol were determined by HPLC and MS.     

The spin delocalization substituent parameter σ˙. 7. Meta-substituent effects on the cyclodimerization of trifluorostyrenes. A test for the σ˙JJ approach

Rate constants (k's) of the thermal cyclodimerization of ten meta-substituted trifluorostyrenes (m-Y-TFS's) have been measured in the temperature range 110–160°C. On the basis of these k's and the σ_mb values derived from ¹⁹F NMR data the spin-delocalization substituent constant σ^˙_m values of these ten meta-substituents have been calculated. The averaged σ^˙_m values are: m-Et, 0.09; m-t-Bu, 0.11; m-F, 0.03; m-Cl,?0.05; m-Br, 0.12: m-CF₃, ?0.07; m-OMe, 0.10; m-NO₂, ?0.002; m-CN, 0.11 and m-CO₂Me, 0.08. Both the smallness of these values and the nonexistence of correlation between Hammett-Type polar σ^X and these σ^˙_m values support our belief that the σ_j?J approach is reliable and trustworthy.     

硒与消化系统癌关系的探讨

据不同地貌、地质条件在30个县市按剖面、同步、随机取土壤样品372份．测定硒等微量元素含量．作等级相关分析显示。土壤硒含量与消化系统癌呈负相关关系．作相对危险度、剂量-效应及多因素分析,认为此负相关关系并非偶然现象．     

Synthesis, structure and heterogeneous catalytic activities of Cu-containing polymeric compounds: anion effect and comparison of homogeneous vs. heterogeneous catalytic activity

The structures of new polymeric compounds containing Cu(II) ions and btp (2,6-bis(N'-1,2,4-triazolyl)pyridine) ligands have been determined. The btp ligands bridge Cu(II) ions to form double zigzag chains, [Cu(ClO4)2(btp)2] 3 with perchlorate anions, and form single zigzag chains, [Cu(btp)(H2O)4](SO4).2H2O 4 with sulfate anions. The polymeric compound 3 was found to effectively catalyze the epoxide ring-opening reaction with methanol, while polymeric compound 4 was almost inactive with epoxides under the same conditions. The polymeric compound 3 showed an efficient catalytic activity and regioselective reactivity in the ring opening of epoxides and allowed reuse without a significant loss of activity through three runs with epoxides.     

对称三唑Schif碱和氯化铜配合物的研究

本文介绍水杨配合与４－氨基－３，５－二乙基－１，２，４－三唑缩合而成对称三唑Ｓｃｈｉｆ碱（ＳＡＥＴＺ）与氯化铜（ＣｕＣｌ２）形成一种新的配合物Ｃｕ（ＳＡＥＴＺ）２（ＳＡＥＴＺ＝４－（邻羟苯基亚甲基）－亚胺－３，５－二乙基－１，２，４－三唑）。配合物的晶体结构表明，分子中两个偶氮甲碱的Ｎ原子及两个酚氧原子与中心Ｃｕ原子形成规则的平面配位结构。晶体属单斜晶系，空间群Ｐ２１／ｎ，ａ＝８．６８８（２），ｂ＝９．３１４（１），ｃ＝１６．５１５（４），β＝９４．３４（２）。，Ｖ＝１３３２．５（７）３，Ｚ＝２。     

Layer by layer buildup of polysaccharide films: physical chemistry and cellular adhesion aspects

The formation ofpolysaccharide films based on the alternate deposition of chitosan (CHI) and hyaluronan (HA) was investigated by several techniques. The multilayer buildup takes place in two stages: during the first stage, the surface is covered by isolated islets that grow and coalesce as the construction goes on. After several deposition steps, a continuous film is formed and the second stage of the buildup process takes place. The whole process is characterized by an exponential increase of the mass and thickness of the film with the number of deposition steps. This exponential growth mechanism is related to the ability of the polycation to diffuse "in" and "out" of the whole film at each deposition step. Using confocal laser microscopy and fluorescently labeled CHI, we show that such a diffusion behavior, already observed with poly(L-lysine) as a polycation, is also found with CHI, a polycation presenting a large persistence length. We also analyze the effect of the molecular weight (MW) of the diffusing polyelectrolyte (CHI) on the buildup process and observe a faster growth for low MW chitosan. The influence of the salt concentration during buildup is also investigated. Whereas the CHI/HA films grow rapidly at high salt concentration (0.15 M NaCl) with the formation of a uniform film after only a few deposition steps, it is very difficult to build the film at 10(-4) M NaCl. In this latter case, the deposited mass increases linearly with the number of deposition steps and the first deposition stage, where the surface is covered by islets, lasts at least up to 50 bilayer deposition steps. However, even at these low salt concentrations and in the islet configuration, CHI chains seem to diffuse in and out of the CHI/HA complexes. The linear mass increase of the film with the number of deposition steps despite the CHI diffusion is explained by a partial redissolution of the CHI/HA complexes forming the film during different steps of the buildup process. Finally, the uniform films built at high salt concentrations were also found to be chondrocyte resistant and, more interestingly, bacterial resistant. Therefore, the (CHI/HA) films may be used as an antimicrobial coating.     

2-硝基丙烯热解反应的理论研究

利用MO-AM1方法研究了2-硝基丙烯热解的反应途径。结果表明, 2-硝基丙烯可能首先热解产生一个四元环状中间体。该中间体依照分步过程继续分解时, 存在两种可能的途径, 其中先断N—O键的反应过程比先断C—C键的过程从能量上更为有利。反应过程中电荷无明显转移, 具有双自由基反应特点。