Novel Monocyclam Derivatives as HIV Entry Inhibitors: Design,Synthesis, Anti‐HIV Evaluation,and Their Interaction with the CXCR4 Co‐receptor

The CXCR4 receptor has been shown to interact with the human immunodeficiency virus (HIV) envelope glycoprotein gp120, leading to fusion of viral and cell membranes. Therefore, ligands that can attach to this receptor represent an important class of therapeutic agents against HIV, thus inhibiting the first step in the cycle of viral infection: the virus–cell entry/fusion. Herein we describe the in silico design, synthesis, and biological evaluation of novel monocyclam derivatives as HIV entry inhibitors. In vitro activity testing of these compounds in cell cultures against HIV strains revealed EC₅₀ values in the low micromolar range without cytotoxicity at the concentrations tested. Docking and molecular dynamics simulations were performed to predict the binding interactions between CXCR4 and the novel monocyclam derivatives. A binding mode of these compounds is proposed which is consistent with the main existing site‐directed mutagenesis data on the CXCR4 co‐receptor. Moreover, molecular modeling comparisons were performed between these novel monocyclams, previously reported non‐cyclam compounds from which the monocyclams are derived, and the well‐known AMD3100 bicyclam CXCR4 inhibitors. Our results suggest that these three structurally diverse CXCR4 inhibitors bind to overlapping but not identical amino acid residues in the transmembrane regions of the receptor.     

炭分子筛的孔径分布研究

采用容积法测定了CO2在两种炭分子筛（CMS-200A、CMS-200B）上的吸附等温线,温度为273K、相对压力为0.000001～0.9。通过HK模型和D-R方程对吸附平衡数据进行分析,计算得到了两种炭分子筛的孔径分布。结果表明：两者的孔径分布主要在0.35～0.8nm之间,CMS-200B的平均孔径略大于CMS-200A。HK模型和D-R方程两种方法均可以反映出两种炭分子筛孔径分布的差异,且计算得到的结论是一致的。     

煤基碳分子筛的制备及CH4/N2分离性能研究

以煤为原料,通过气相碳沉积法制备了CH4/N2变压吸附分离用碳分子筛,研究了苯沉积量对碳分子筛吸附性能的影响。用液氮吸附（77 K）、扫描电镜对碳分子筛孔结构及表面形貌进行了表征,结果表明：制备的碳分子筛（CMS-1）平衡分离系数大于5,比表面积SBET=251.5 m2/g,微孔孔容Vm=0.1178 mL/g,孔径主要分布在0.35~2 nm,能满足CH4/N2变压吸附分离要求。     

紫外辐照交联改性UHMWPE纤维的研究

选取不同生产阶段的超高相对分子质量聚乙烯(UHMWPE)纤维进行紫外辐照交联改性,探讨了正庚烷浸泡时间、交联剂浓度、紫外辐照时间等因素对交联效果、纤维力学性能及蠕变性能的影响.结果表明:UHMWPE纤维在正庚烷中的最佳浸泡时间为48 h;紫外光最佳辐照改性时间为6 min;与初生纤维和成品纤维相比,相同改性条件下冻胶纤...     

低分子量聚丙烯酸钠的合成及应用

采用溶液聚合方法合成低分子量聚丙烯酸钠,得出制取低分子量聚丙烯酸钠的最佳适宜条件为：单体用量25 g、引发剂用量为单体用量的7%、链转移剂用量7.5 g、聚合温度为80℃。     

污水生物处理系统中溶解性微生物产物的研究进展

对SMP的定义、来源、组成、特性、影响因素、动力学模型以及SMP诱导的膜污染和控制措施进行了总结.SMP是由于基质新陈代谢和生物量衰减释放到溶液中的一类有机化合物,其主要组成为腐植酸和富里酸、多糖、蛋白质、核酸、有机酸、氨基酸、抗生素、类固醇、胞外聚合酶、含铁细胞等.这些物质大都具有一定的毒性和螯合金属的能力,在MBR系统中还会引发膜污染.研究证明活性炭吸附对SMP的去除效果最佳.     

高分子表面活性剂的合成

以丙烯酸、丙烯酰胺和丙烯酸丁酯为单体,采用瞬时聚合法合成了高分子表面活性剂。表面活性研究表明,制备的高分子表面活性剂有良好的表面活性,表面张力可低至42 mN/m。红外光谱表明,产物没有发生交联,黏度法测定产物的分子量为2×104～4×104。     

塑料摩擦试验方法的研究

以尼龙和超高分子量聚乙烯为研究对象,寻求一种理想的摩擦试验用试样预处理方法;并研究塑料在钢上滑动和钢在塑料上滑动的两种摩擦类型的摩擦系数区别及关系。通过反复性试验发现,采用砂纸预处理螺纹状试样,并与螺纹状摩擦副配套使用,摩擦面积和稳定性都大幅度增加;两种不同的滑动方式所得到的摩擦系数相差很大,具有不可比性。     

先进光刻胶材料的研究进展

本文简述了光刻技术及光刻胶的发展过程,并对应用于193纳米光刻和下一代EUV光刻的光刻胶材料的研究进展进行了综述,特别对文献中EUV光刻胶材料的研发进行了较为详细的介绍,以期对我国先进光刻胶的研发工作有所帮助.     

不同结晶度纤维素的酶解历程的SEC-MALLS研究(英文)

The reactions of exo-cellulase (cellobiohydrolase, CBH) and endo-cellulase (endoglucanase, EG) were investigated by analyzing the insoluble residues of microcrystalline cellulose (MCC) and filter paper cellulose (FPC) during enzymatic hydrolysis. Molecular parameters including molecular weight and its distribution, degree of po-lymerization, and radii of gyration were measured by size exclusion chromatography coupled with multi-angle laser light scattering. No significant change in MCC chains was found during the whole reaction period, indicating that CBH digestion follows a layer-by-layer solubilization manner. This reaction mode might be the major reason for slow enzymatic hydrolysis of cellulose. On the other hand, the degree of polymerization of FPC chains decreases rapidly in the initial reaction, indicating that EG digestion follows a random scission manner, which may create new ends for CBH easily. The slopes of the conformation plots for MCC and FPC increase gradually, indicating stronger chain stiffness of cellulose during hydrolysis.