吲哚席夫碱类衍生物的合成及其抗HIV-1活性研究

设计、合成吲哚席夫碱类衍生物并研究其抗HIV-1活性。以3-吲哚甲醛衍生物为原料,在碱催化下与芳香胺发生缩合反应合成吲哚席夫碱类化合物,并采用通过 MTT 法测试了目标化合物在MT-4 细胞内的抗 HIV-1病毒株的活性。 合成了32个吲哚席夫碱类衍生物,其结构均通过1H NMR和MS加以确证。初步的生物活性结果测试表明,所合成的吲哚席夫碱类化合物对HIV-1均有优秀的抑制活性,并具有广谱的抗HIV-1活性。其中化合物31 (EC50 = 0.06 mol/L)展现出了最强的抗HIV-1活性,与阳性药物地拉韦啶 (DLV, EC50 = 0.57 mol/L)相当;同时,化合物31具有非常低的毒性,选择指数 (SI)高达2500,明显高于地拉韦啶 (DLV, SI = 1272.9)和依法韦仑 (EFV, SI = 321)。将吲哚和席夫碱两个药效团,能够得到高效、低毒的HIV-1逆转录酶抑制剂,为今后发展新型的HIV-1抑制剂提供了新思路。     

Efficient cycloaddition of CO2 and epoxides to cyclic carbonates using salen-based covalent organic framework as a heterogeneous catalyst

Journal of Porous Materials - Salen-based covalent organic framework (COF), constructed by salen skeleton, has great potential applications as the heterogeneous catalyst due to its unique...     

Biodegradable,superhydrophobic walnut wood membrane for the separation of oil/water mixtures

The preparation of environmentally friendly oil/water separation materials remains a great challenge. Freeze-drying of wood after lignin removal yields wood aerogels, which can be used as substrates to prepare fluorine-free environmentally friendly superhydrophobic materials, However, they are more suitable for absorption rather than filtration applications due to their poor strength. A study using cross-sections of pristine wood chips as substrates retains the original strength of wood, but the use of the cross-sectional of wood pieces limits their thickness, strength, and size. In this paper, a degradable fluorine-free superhydrophobic film (max. water contact angle of approximately 164.2°) with self-cleaning and abrasion resistance characteristics was prepared by a one-step method using pristine and activated walnut longitudinal section films as the substrate, with tetraethyl orthosilicate as a precursor and dodecyltriethoxysilane as a modifier. The tensile strength results show that superhydrophobic films with pristine or activated wood substrates maintained the strength of pristine wood and were 2.2 times stronger than the wood aerogel substrate. In addition, after cross-laminating the two samples, the films had the ability to separate oil and water by continuous filtration with high efficiency (98.5%) and flux (approximately 1.3 × 10³ L∙m^‒2∙h^‒1). The method has potential for the large-scale fabrication of degradable superhydrophobic filtration separation membranes.     

UPLC-MS/MS法测定美洛昔康中两个中间体杂质

建立UPLC-MS/MS法测定美洛昔康中杂质A和杂质B.采用ACQUITY UPLC?HSS T3 C18(2.1 mm×100 mm,1.8μm)色谱柱,流动相为0.1％甲酸水溶液-甲醇(45:55).采用电喷雾离子源(ESI),多反应监测(MRM)模式,正离子扫描;脱溶剂温度:500℃;干燥气流速:15 L/min...     

季铵盐缓蚀剂在高温高压电化学环境下缓蚀行为研究

在油气田的开发和运营中,设备和管道面临着严苛的腐蚀环境,绝大多数研究只针对缓蚀剂在常温常压的缓蚀行为,而对于高温高压环境下这种实际应用环境的缓蚀剂开发和研究较少.基于以上问题,选用并制备两种季铵盐缓蚀剂,使用电化学高温高压釜模拟油气田环境,通过电化学方法以及SEM和EDS表征,研究了N80钢在模拟油气田环境下的电化学行...     

TS法的改进及其在求解化工优化问题中的应用

TS算法属于现代优化算法,是局部领域搜索法的推广,常用于求解组合优化问题.利用TS法搜索过程的有向性和能够跳离局部最优解的特点,对其进行了改造,以适应求解连续变量化工优化问题.首先,根据化工优化问题变量的特性,提出了一种简便的邻域映射方案,并改进了迭代过程中自适应因子的下降函数;进一步分析对比了禁忌步数、自适应因子和初始解等参数对于优化结果的影响.然后通过算例和换热网络优化问题的求解,表明改造后的TS法在求解连续变量化工优化问题中的有效性,及其在化工优化领域的发展价值.     

基于案例推理的HAZOP分析自动化框架

危险与可操作性（HAZOP）分析是一种广泛应用于化学流程工业的危险分析方法。为克服现有的HAZOP分析专家系统在“非常规”分析方面的局限性,提出了基于案例推理（CBR）的HAZOP分析自动化方法,描述了案例库及案例结构,给出了案例搜索策略。为便于案例库的知识管理,开发了案例构造器。工业实例应用结果表明,基于CBR的HAZOP专家系统突破了现有HAZOP专家系统没有学习能力和不能进行“非常规”分析的技术瓶颈。     

Isothermal crystallization kinetics and melting behavior of multiwalled carbon nanotubes/polyamide‐6 composites

Pristine and functionalized multiwalled carbon nanotubes (MWNTs) were used to fabricate polyamide 6 (PA6) composites through melt blending. The functionalized MWNTs were obtained by grafting 1,6‐hexamethylenediamine (HMD) onto the pristine MWNTs to improve their compatibility with PA6 matrix. The effect of MWNTs on the isothermal crystallization and melting behavior of PA6 was investigated by differential scanning calorimetry (DSC) and X‐ray diffraction (XRD). The Avrami and Lauritzen–Hoffmann equations are used to describe the isothermal crystallization kinetics. The values of the Avrami exponent found for neat PA6, the pristine MWNTs/PA6 and functionalized MWNTs/PA6 composite samples are about 4.0, 1.7, and 2.3, respectively. The activation energies are determined by the Arrhenius method, which is lower for the composites, ?320.52 KJ/mol for pristine MWNTs/PA6 and ?293.83 KJ/mol for functionalized MWNTs/PA6, than that for the neat PA6 (?284.71 KJ/mol). The following melting behavior reveals that all the isothermally crystallized samples exhibit triple melting endotherms at lower crystallization temperature and double melting endotherms at higher crystallization temperature. The multiple melting endotherms are mainly caused by the recrystallization of PA6 during heating. The resulting equilibrium melting temperature is lower for the composites than for neat PA6. In addition, polarizing microscopy (PLM) and small angle light scanning (SALS) were used to study the spherulite morphology. The results show that the MWNTs reduce the spherulite radius of PA6. This reduction is more significant for pristine MWNTs. © 2007 Wiley Periodicals, Inc. J Appl Polym Sci 2007