Enantioselective Aldol Reaction between Isatins and Ketones,Catalyzed by Chiral Norephedrine-Derived β-Amino Alcohols with a Thiophene Moiety

Russian Journal of Organic Chemistry - Chiral norephedrine-based β-amino alcohol bearing a substituted thiophene ring were applied as catalysts for the enantioselective aldol reaction of...     

Synthesis of N‐Alkylated Indolines and Indoles from Indoline and Aliphatic Ketones

A survey of redox aminations of indoline with aliphatic ketones using bismuth nitrate as catalyst is described. A reaction of an equivalent amount of indoline and aliphatic cyclic and acyclic ketones provides a mixture of excessive alkylated indole derivatives over typically redox isomerization and reductive alkylation pathways while using of the five equivalent of indoline provides N‐alkylated indolines as a reductive alkylation product. The desired N‐alkyl indoles from the oxidation of N‐alkyl indolines were obtained in excellent yields.     

Redox Amination Scope of Benzylic Ketones with Indoline: Synthetic and Mechanistic Insights

Bi(NO₃)₃·5H₂O‐Catalyzed redox amination scope and mechanistic insights of benzylic ketones with indoline are discussed. The experimental results demonstrate that the formation of N‐alkyl‐substituted indole/indoline derivatives over typically competitive redox and reductive amination processes is depending upon the reaction condition for the benzylic ketones.     

基于电磁振动上料的茶梗和昆虫异物近红外光谱和荧光图像在线检测研究

茶叶是大众青睐的健康饮品之一,但茶叶在机器采收和加工过程中,容易混入茶梗和昆虫异物,污染茶叶、影响其质量安全,是未来应防范和检测的重点。X射线成像技术,根据食品基质和异物的密度差实施检测,广泛适用于金属异物并延伸至高密度塑料,但对于茶梗、昆虫这类低密度有机异物尚不适用,所以迫切需要研发新型无损检测技术和方法。针对片状茶叶重叠、遮掩异物的问题,提出了电磁振动上料辅助近红外光谱和荧光图像的检测方案,进行绿茶中的内源性异物茶梗和外源性异物昆虫的在线检测研究。通过电磁振动上料辅助近红外光谱和荧光成像系统,采集了600～1 050 nm范围的近红外光谱600条和RGB-N四通道图像各65幅。采用451条光谱进行建模,其余149条光谱作为预测集,评估模型的性能,比较了去趋势(Detrending)、多元散射校正(MSC)、标准正态变换(SNV)、变权重正态变换(VSN)、迭代自适应加权惩罚最小二乘法(airPLS)、不对称最小二乘法(ALS)、光程估计与校正(OPLEC)等不同光谱预处理方法的处理效果,其中OPLEC能较好地消除散射效应,偏最小二乘判别分析(PLS-DA)模型的正确识别率由78%提...     

Pharmacological properties of dicyanidoaurate(I)-based complexes: characterization and single crystal X-ray analysis

The synthesis of three bimetallic cyanido complexes with edbea [2,2′-(ethylenedioxy)bis(ethylamine)] ligand is reported. [Ni^II(μ-edbea)₂{Au(μ-CN)₂}₂]_n (1), [{Cu^II(edbea)}₂{Au(μ-CN)₂}₄]_n (2) and [Cd^II(edbea)₂][Au(CN)₂]₂·H₂O (3) were fully characterized by elemental, infrared, XRD (3), ESI-MS and thermal analysis. The DNA/BSA binding properties of these complexes were evaluated by spectrophotometric titration, fluorometric ethidium bromide kinetics, and DNA electrophoresis studies and their partially minor groove binding mode between the base pairs of DNA and electrostatic interaction between the amino acid residues of BSA were explained. The complexes were tested for their pharmacological properties. These molecules had excellent in vitro antiproliferative activity and also exhibited a strong tumor inhibiting effect against HT29, HeLa, C6 and Vero cell lines. These complexes had metastatic features as they are able to reduce cell migration activity and suppress tumor growth in vitro. Analysis of the DNA topoisomerase I relaxing activity indicates that the complexes do not inhibit topoisomerase I which regulates the topological states of the DNA double helix during DNA processing reactions. The TUNEL and DNA laddering assay results indicated that these compounds may destroy cell maintenance by triggering apoptosis. Immunohistochemistry staining analysis demonstrated that these complexes significantly decreased the expression of Bcl-2 in HeLa and HT29 cells while increasing the expression of P53 levels. Overall, the potent antiproliferative activity, low cytotoxic effect, good solubility, and micro molar range dosage observed for these complexes emphasizes their potential as anticancer drug candidates.     

Dual Reciprocity Boundary Element Method for Magnetohydrodynamic Flow Using Radial Basis Functions

A dual reciprocity boundary element method is given to obtain the solution in terms of velocity and induced magnetic field for the study of MHD (magnetohydrodynamic) flow through a rectangular duct having insulating walls. The equations are transformed to two types of nonlinear Poisson equations and the right-hand sides in these equations are approximated using combinations of two classes of radial basis functions (the value of the function and its normal derivatives are utilized for approximation). Computations are carried out for several values of the Hartman number (0 h M h 10) by using constant boundary elements. Comparisons are made for two types of formulations and for traditional and osculatory type approximations of the right-hand side functions. It is found that osculatory interpolation gives better results than traditional interpolation and the type of the Poisson equation, which contains derivative of the unknown function, is better than the other type, which contains unknown function only. The results for velocity and induced magnetic field are illustrated by some selected graphs.     

Development of a solid‐phase microextraction LC–MS/MS method for determination of oxidative stress biomarkers in biofluids

Recently the connection between oxidative stress and various diseases, including cancer and Alzheimer's, attracts notice as a pathway suitable for diagnostic purposes. 8‐Oxo‐deoxyguanosine and 8‐oxo‐deoxyadenosine produced from the interaction of reactive oxygen species with DNA become prominent as biomarkers. Several methods have been developed for their determination in biofluids, including solid‐phase extraction and enzyme‐linked immunosorbent assays. However, still, there is a need for reliable and fast analytical methods. In this context, solid‐phase microextraction offers many advantages such as flexibility in geometry and applicable sample volume, as well as high adaptability to high‐throughput sampling. In this study, a solid‐phase microextraction method was developed for the determination of 8‐oxo‐deoxyguanosine and 8‐oxo‐deoxyadenosine in biofluids. The extractive phase of solid‐phase microextraction consisted of hydrophilic–lipophilic balanced polymeric particles. In order to develop a solid‐phase microextraction method suitable for the determination of the analytes in saliva and urine, several parameters, including desorption solvent, desorption time, sample pH, and ionic strength, were scrutinized. Analytical figures of merit indicated that the developed method provides reasonable interday and intraday precisions (<15% in both biofluids) with acceptable accuracy. The method provides a limit of quantification for both biomarkers at 5.0 and 10.0 ng/mL levels in saliva and urine matrices, respectively.