Tentoxin as a scaffold for drug discovery. Total solid-phase synthesis of tentoxin and a library of analogues

[reaction: see text] A solid-phase method for the synthesis of tentoxin has been developed. Two key steps-dehydration and N-alkylation-are carried out while the peptide is anchored to the resin. The method, which has been validated by the preparation of a library of tentoxin analogues, should be applicable to the generation of further libraries that have the tentoxin scaffold structure, as well as other structures containing N-alkylated didehydroamino acids.     

The Potential Energies of Cohesion of a Crystalline Organic Enantiomer and the Racemate; on the Energy for the Liquid Racemate [1]

The cohesion potential energy of the crystal of one enantiomer of ethyl 3-cyano-3-(3,4-dimethyloxyphenyl)-2,2,4-trimethylpentanoate, −47.7 ± 0.1 kJ mol⁻¹ (0–90°C), was found out from the heat of sublimation (123.2 ± 5.1 kJ mol⁻¹, 78.6°C) and the kinetic energies for the gas phase and the crystal. It was found that the entropy function of Debye’s theory of solids mathematically agreed with the vibrational entropy of the gas (variationally obtained), allowing to disclose the vibrational energy using the Debye energy function (E _vib 835.0 kJ mol⁻¹ (78.6°C), E ⁰ included). E _kin for the crystal (771.1 kJ mol⁻¹ (78.6°C)) was obtained by Debye’s theory with the experimental heat capacity. The cohesion energy represented a moderate part of the sublimation energy. The cohesion energy of the racemic crystal, −44.2 kJ mol⁻¹, was obtained by the heat of formation of the crystal in the solid state (3.0 kJ mol⁻¹, 83.3°C) and E _kin for the crystal (by Debye’s theory). The decrease in cohesion on formation of the crystal accounted for the energy of formation. The change in potential energy on liquefaction of the racemate from the gas state was disclosed obtaining added-up E _{vib + rot} for the liquid in the way as to E _vib for the gas, the Debye entropy function being increasedly suited for the liquid (E _{vib + rot} 763.4 kJ mol⁻¹ (115.4°C)). Positive ΔE _pot, 13.0 kJ mol⁻¹, arised from the increase in electronic energy (Δ _l ν_mean − 154.3 cm⁻¹, by the dielectric nature of the liquid), added to the cohesion energy.     

Modular bis(oxazoline) ligands for palladium catalyzed allylic alkylation: unprecedented conformational behaviour of a bis(oxazoline) palladium eta3-1,3-diphenylallyl complex

New families of enantiopure bis(oxazolines) with 4,5-trans (5 a-g) or 4,5-cis (6 c) stereochemistry at the individual rings have been prepared in high yield. Their eta(3)-allyl palladium complexes (8 a-g, 9 c and 10) have been used as catalytic precursors in allylic alkylation reactions with excellent enantioselectivities (up to 96 %) for the trans oxazoline derivatives, while Pd/6 c system was inactive. NMR studies on palladium eta(3)-1,3-diphenylallyl intermediates (11 a, c and e) showed the presence of syn/syn- and syn/anti-allyl isomers in solution; this resembles the first example of eta(3)-eta(1)-eta(3) isomerism in Pd allylic complexes containing bis(oxazolines) derived from malonic acid.     

单片机多机通信中中间通信机的设计

介绍了单片机树型网络多机通信系统的结构及一种用两片单片机AT89C52的双CPU电路方案实现树型网络多机通信中中间通信机的新方法．     

光子晶体的制备及其应用

介绍了光子晶体的基本概念、主要特征及其制备方法和应用前景。     

晋城市政府局域网的建设与应用

详细介绍了晋城市政府Intranet网络建设的方案及其应用，总结和提出了网络建设过程中应该引起注意的一些问题。     

基于混沌-量子粒子群的分簇路由算法

针对粒子群分簇路由优化算法存在的收敛速度慢、 易陷入局部最优等问题, 提出一种混沌-量子粒子群 的双子粒子群分簇路由算法。 该算法以簇头的能量、 簇头与汇聚节点的距离以及与簇内成员节点的距离构造 最优簇头的代价函数, 主粒子群利用混沌粒子群寻优, 辅粒子群利用量子粒子群寻优, 加入量子波动理论, 使 算法具有较好的全局收敛性。 双子粒子群采用收敛速度快的凹函数递减策略优化权重。 仿真结果验证了该算 法可使无线传感网络节点能量消耗均衡化, 显著延长网络生命周期, 与 LEACH(Low-Energy Adaptive Clustering Hierarchy)协议、 PSO-C(Cluster setup using Particle Swarm Optimization algorithm)协议相比生命周期分别延长了 80. 1%和 41. 4%。     

基于改进 FastICA 的冲击波工频干扰消除算法

在火炮冲击波信号测试领域中, 为解决陷波算法消除工频干扰损失有效信号成分的问题, 提出了一种改 进的 FastICA 算法消除工频干扰。 采用五阶收敛的牛顿迭代形式改进基于负熵的 FastICA 算法, 使其不仅具备 负熵算法的高精准度, 而且收敛速度快, 迭代次数少。 仿真结果表明, 该算法的相似系数和信噪比达到 0. 999 99和 45 dB, 较传统陷波算法的 0. 996 和 21 dB 有明显的优势。 相比于基于负熵的 FastICA 算法, 改进算 法与其精准度相同, 但迭代次数减少了 26. 7%; 与收敛速度较快的峭度算法相比, 改进算法迭代次数更少, 收 敛速度更快, 稳定性更高。 该算法具备精准度高、 收敛速度快和迭代次数少等优势, 因此适用于实时处理冲击 波的测试场合。     

正硅酸四乙酯改性活性炭电极材料及其电化学性能测试研究

以正硅酸四乙酯(TEOS)为改性剂,在常温下对竹炭表面处理,并对处理前后的材料进扫描电子显微镜(SEM)、N_2吸脱附、傅立叶转换红外线光谱(FTIR)等结构表征。将改性材料制成电极,以1 mol/L Na_2SO_4为电解液进行循环伏安(CV)、交流阻抗和恒流充放电等测试;其结果显示,在20 mV/s的扫描速率下,经0.50%的TEOS改性的竹炭中制成的电极材料的电化学性能较好。与改性前相比,当电流密度为1 A/g时,比容量达到76.5 F/g,比电容提高了80%。TEOS改性成本较低,简便易行,效果显著。     

玉米芯基活性炭吸附去除水中重金属的实验及机理研究

运用农作物废弃物玉米芯为原料,通过马弗炉在不同工艺条件下碳化制备玉米芯基活性炭,考察了其对锌、锰和铅三种重金属的吸附性能,并利用傅里叶红外光谱、扫描电镜(SEM及EDS)等手段研究了其吸附重金属锌的机理,并对吸附后的吸附剂进行解吸实验.实验结果表明,合适工艺下生产的玉米芯基活性炭对水中锌离子有极高的吸附率,吸附动力学行为符合准二级动力学方程;对玉米芯基活性炭的解吸,酸解吸法比电场干预解吸法能取得更好的效果.初步判断玉米芯基活性炭可用于吸附重金属,是一种低成本吸附剂.