Study on Inhibitors of Methionine Synthase Ⅷ: Synthesis of 2,5-Diamino-4-oxo-6- (3-butenyl) pyrimidine

Cobalamin-dependent methionine synthase plays a crucial role in folate metabolism and such would appear to be an excellent target for rational antifolate drug design. However, to date, no anticancer agents directed at this enzyme are available, but the enzyme is efficiently and specifically inhibited by N2O and this has proven invaluable for evaluating the biochemical consequence of enzyme inhibition and for mechanistic studies. [1,2] 2,5-Diamino-4-oxo-6-(3-butenyl) pyrimidine, a key intermediate in synthetic inhibitors of methionine synthase, was first synthesized using γbutenyl-β-ketoester and guanidine carbonate (Scheme 1). [3]     

Triterpenoid Constituents of Huperzia miyoshiana

Thirteen triterpenoids, including three new ones, miyoshianois A (1), B (2) and C (3), were isolated from Huperzia miyoshiana. The structures of these new compounds were established as 3-O-dihydroferuloyltohogenol (1), 16-oxo-3β,21β-dihydrox-y-serrat-14-en-24-ferulate (2) and 16-oxo-3a, 21β-dihydroxy-serrat-14-en-24-ferulate (3), respectively, on the basis of their spectroscopic analysis.     

A novel strategy to verification of adulteration in alcoholic beverages based on Schlieren effect measurements and chemometric techniques

A novel strategy to evaluation of adulteration in alcoholic beverages based on the measurement of the Schlieren effect using an automated FIA system with photometric detection is proposed. The assay is based on the Schlieren effect produced when beverage samples are injected in a single-line FIA system that uses water as carrier stream and a light-emitting diode-phototransistor photometer controlled by microcomputer as detector. The flow system presents limited mixing conditions which make possible to create gradients of refractive index (Schlieren effect) in the injected sample zone. These gradients are reproducible, characteristic of each alcoholic beverage and undergo specific modifications when adulterations with water or ethanol are imposed. Schlieren effect data of brandies, cachaças, rums, whiskies and vodkas were treated by SIMCA to elaborate class models applied in the evaluation of alcoholic beverages adulteration. Samples of the original matrix of each sort of beverages were adulterated in laboratory by adding water, methanol and ethanol in levels of 5% and 10% (v/v). These samples were used as test set to validate SIMCA class models. The verification of authenticity using Schlieren effect measurements presented good results making possible to identify 100% of the beverages samples adulterated in laboratory and 93% of the actual adulterated alcoholic beverages with confidence levels of 95%. As principal advantage, the automated system does not use reagents to carry out the analysis.     

聚己内酯与不同纤维素衍生物形成的共混体系的红外光谱研究

用傅里叶变换红外光谱研究了聚己内酯与硝基纤维素、乙基纤维素和纤维素氨基甲酸酯所形成的共混体系中组分间的相互作用。对羟基基团、羰基基团以及聚己内酯结晶相相关的吸收谱带分析表明 :随着纤维素结构单元上羟基被取代程度的增加 ,纤维素衍生物的自身氢键相互作用明显减弱 ,而与聚己内酯之间的相互作用得到加强。这种相互作用的加强 ,显著改变了聚己内酯的结晶行为 ,使其结晶能力减弱。     

Possible triggering of solar activity to big earthquakes (Ms ≥ 8) in faults with near west-east strike in China

A big earthquake (Ms = 8.1) occurred at western Kunlun Mts gap on November 14, 2001. It is the biggest earthquake in China in the past 50 years and the only one with a magnitude bigger than 8 in China after Dangxiong Earthquake (M = 8) in Tibet in 1951. The big earthquake has drawn wide attention of scientists in seismological, geophysical, geological and astro-geodynamic circles. Scientists are interested in the occurrence regularity of the very big earthquakes and try to find out the fac…     

Three Stilbene Tetramers from the Roots of Caragana sinica

Three stilbene tetramers, carasinols A-C (1-3), along with three known substances, leachianol C, cararosinol A and stenophyllol B, were isolated from the roots of Caragana sinica. Their structures were elucidated by spectroscopy. It was found that compounds isolated except for stenophyllol B stimulated the proliferation of cultured osteoblasts.     

Penta-Coordinate Phosphorus Intermediates Analysis on Phospho-related Proteins

In this paper, based on known crystal structures of square pyramid （SP） and trigonal bipyramid （TBP） penta coordinated phosphorus compounds containing amino acid side chains, such as amino, carboxyl, hydroxyl or thiol, a software for survey the P（5）-structure of phosphorylated proteins was derived. By this software, it was found that 382 of 398 phosphorus related kinases （96%） from current PDB could go through the penta-coordinated phosphorus transition state or intermediate.     

二阶拟线性椭圆型方程振动性的积分平均方法

§ 1.　IntroductionThepurposeofthispaperistostudytheoscillatorybehaviorofsolutionsofcertainquasi linearellipticequationsdiv( ｜Du｜m -2 A(x)Du) + p(x) ｜u｜m -2 u=0 ,x∈Ω Rn,(E)whereΩisanexteriordomain ,m >1 ,andfunctionsA(x) ,p(x)aretobespecifiedinthefollowingtext.Recently ,USAMI [6]consideredEq .(E)whenA(x)≡I (identitymatrix) ,andob tainedoscillationcriteriaforEq .(E)with“infiniteintegral”coefficient [cf.[6],Theorem 4].However,asfarasthepresentreferencesisconcerned ,therearefewo…     

基于突变论的林火蔓延分析

在对森林火灾进行能量和质量守恒分析的基础上,把尖点突变模型应用于森林火灾蔓延的预测,使突变理论在 森林火灾的模型中从理论上有了初步的应用。文中计算了林火发生突变时的一些分歧点,分析了林火突变的特点和变化规 律。     

Na离子和Cl离子引起He原子直接多重电离过程的研究

利用2～8 MeV的Naq+、Clq+(q=2,3,4,5)轰击氦原子,对碰撞的直接多重电离过程进行研究.实验采用反冲离子-散射离子飞行时间符合技术,通过反冲离子飞行时间谱区分不同价态反冲离子;利用静电偏转和位置灵敏探测技术区分不同电荷态散射离子;结合CAMAC-PC多参数获取系统得到一定价态散射离子所对应的反冲离子电荷态分布谱;经分析该谱得到直接多重电离截面与直接单电离截面之比R21.讨论了R21随入射离子速度和电荷态的变化关系.