Synthesis and In Vitro Anti-HIV Activity of Some New Schiff Base Ligands Derived from 5-Amino-4-phenyl-4H-1,2,4-triazole-3-thiol and Their Metal Complexes

New Schiff base ligands (6–9) derived from 5-amino-4-phenyl-4H-1,2,4-triazole-3-thiol 1 and substituted benzaldehydes (2–5) as well as their metal complexes with Cu(II), Fe(II), Au(III), and Mn(II) (12–17) have been synthesized. A new benzothiazole derivative (11) was prepared from coupling of 7 with N-(benzothiazol-2-yl)-2-chloroacetamide 10. Their spectral properties were investigated. The newly designed and synthesized Schiff base ligands and the metal complexes were assayed for anti-HIV-1 and HIV-2 activity by examination of their inhibition of HIV-induced cytopathogenicity in MT-4 cells. Compounds 11 and 16 were found to be the most active inhibitors in cell culture (EC₅₀ = 12.2 μg/mL (SI = 4) and > 2.11 μg/mL (SI = > 1), respectively) against HIV-1, whereas 11 showed inhibition against HIV-2 of EC₅₀ > 10.2 μg/mL with SI = 9, which provided a good lead for further optimization.     

黄渤海近岸海域酚类内分泌干扰物分布特征及其来源解析

在黄渤海近岸海域采集了34个水体样品,利用HPLC-MS/MS分析了双酚A、辛基酚、壬基酚、2,4-二氯酚、对叔丁基苯酚和对特辛基苯酚等6种酚类内分泌干扰物的含量,并探讨了其分布特征及来源.结果表明,中国北部近岸海域6种酚类内分泌干扰物的含量范围在5.25～1351.20ng/mL之间.结合因子分析和层次聚类分析结果,说明渤海、黄海近岸海域中酚类化合物主要以辛基酚、壬基酚、2,4-二氯酚为主,局部海域伴有双酚A的高残留;从整个海域范围看,黄渤海近岸海域水体中酚类化合物污染状况具有区域特征,整体呈现出南高北低的特点,且酚类物质分布具有明显的地区特性,一定程度上具有聚集性;来源解析结果表明黄渤海近岸海域中酚类内分泌干扰物主要来源为生活污水和工业废水.     

Novel Uncatalyzed Hydrocyanation of Ketones utlizing Tetrachlorosilane–Potassium Cyanide Reagent

A combination of tetrachlorosilane and potassium cyanide (in situ trichlorosilyl cyanide) was found to work efficiently for hydrocyanation of ketones to afford the corresponding cyanohydrins in high yield under mild conditions.     

Polymers-Copolymer as Flow Improvers for Fuel Oils and Their Electrical Conductivity

In order to find efficient cold flow improvers for fuel oil, polymethylmethacrylate (PMMA), polystyrene (PS), and a copolymer [styrene (S)–methylmethacrylate (MMA) were prepared. The structure of these polymers and the copolymer were characterized by infrared spectral analysis and their molecular weights were measured. These polymers-copolymer were used as additives for fuel oils in order to lower their pour point. Accordingly, they were evaluated as flow improvers for fuel oil. The results indicated that PMMA possesses less performance as pour point depressant. While the addition of PS and the copolymer (S–MMA) yield excellent pour point depressants for fuel oil. Upon studying the prepared additives and their properties, it was found that the electrical properties of the copolymer were changed due to the presence of polar ion in MMA effect on the electrical properties. The highest electrical conductivity was found when styrene:MMA molar ratio was 1:1.     

气相色谱法测定海洋沉积物中十氯酮残留

研究了提取溶剂效率、毛细管柱极性、净化条件及共溶出干扰物等因素对十氯酮测定的影响;对比了加速溶剂提取及超声波提取方式,考察了DB-17、DB-1701与DB-5毛细管柱分离度,及不同比例甲醇/正己烷混合溶液作为定容溶液的分析结果。建立了加速溶剂萃取,H2SO4净化分离,DB-5毛细管柱电子捕获检测器(ECD)-气相色谱法(GC)测定海洋沉积物介质中有机氯农药类持久性有机污染物十氯酮残留分析方法。将5 g沉积物干样与3 g活化铜粉及3 g无水Na2SO4混匀后,采用二氯甲烷-丙酮(1∶1,V/V)进行加速溶剂萃取;萃取液浓缩后,用H2SO4净化,以1%甲醇-正己烷混合溶液定容后,采用DB-5非极性毛细管柱,及配备电子捕获检测器气相色谱测定十氯酮含量。本方法采用外标法进行定量分析,在0.005～0.1 mg/L浓度范围内,线性相关系数为0.9989;加标回收率为75%～98%;相对标准偏差为3.7%～9.6%(n=6);检出限为0.12 ng/g。     

Electrospun copper oxide nanoparticles as an efficient heterogeneous catalyst for N-arylation of indole

The N-arylation of indoles with a variety of aryl bromides is reported using copper oxide nanoparticles as a heterogeneous catalyst. These copper oxide nanoparticles, which were produced in a novel, facile, and scalable fashion via an electrospinning technique, resulted in an excellent product yield under mild conditions. Moreover, the catalyst was easily recovered and reused several times without significant loss of activity.     

Organotin(IV) Carboxylates of Substituted α‐Cinnamic Acid,RnSn(OCOC(R2)=CHR1)4 – n: Synthesis,Spectroscopic Characterization and Biological Evaluation

Di‐ and triorganotin(IV) carboxylates, R_nSn(OCOC(R²)=CHR¹)_4–n (n = 2 and 3; R = Me, Et, n‐Bu, Ph; R¹ = 3‐CH₃O‐4‐OHC₆H₃, R² = C₆H₅) were prepared by reacting the corresponding organotin(IV) chloride with the silver salt of the (E)‐3‐(4‐hydroxy‐3‐methoxyphenyl)‐2‐phenylpropenoic acid. The title compounds were investigated and characterized by elemental analysis, infrared (FT‐IR), multinuclear (¹H, ¹³C, ¹¹⁹Sn) NMR, and mass spectrometry, and possible structures were proposed. The complexes and ligand acid ( HL ) have been evaluated in vitro against various bacteria and fungi. The results noticed during the biocidal activity screenings proved their in vitro biological potential. They were also tested for cytotoxicity.     

二甲基亚砜对乙酸气相色谱保留时间的影响及其机理

通过气相色谱、红外光谱分析和量子化学计算,探究溶于二甲基亚砜（DMSO）中乙酸保留时间发生波动的原因。 结果显示,乙酸保留时间变化与DMSO体积等量递增呈线性关系,R²=0.99301;根据红外光谱分析得出,DMSO和乙酸之间生成了氢键,以DMSO-乙酸分子的形式通过色谱柱;根据Gaussian09程序计算结果,DMSO电子密度大的部分给予电子,与乙酸之间形成了氢键,而DMSO电子密度小的部分容易获得电子与具有强偶极矩的色谱柱固定液聚乙二醇产生作用力,吸附在固定液上。因此,在上述一系列复杂的分子间作用力的共同影响下,乙酸保留时间发生了波动,且随着溶剂DMSO体积比增加,乙酸保留时间不断延长。     

Biogenic Synthesis of Gold Nanoparticles on a Green Support as a Reusable Catalyst for the Hydrogenation of Nitroarene and Quinoline

Direct attachment of gold nanoparticles to a green support without the use of an external reducing agent and using it for removing toxic pollutants from wastewater, i. e., reduction of nitroarene to amine, are described. A novel approach involving the reduction of gold by the jute plant (Corchorus genus) stem-based (JPS) support itself to form nanoparticles (AuNPs) to be used as a catalytic system (‘dip-catalyst’) and its catalytic activity for the hydrogenation of series of nitroarenes in aqueous media are presented. AuNPs/JPS catalyst was characterized using SEM, UV-Vis, FTIR, TEM, XPS, and ICP-OES. Confined area elemental mapping exhibits uniform and homogeneous distribution of AuNPs on the support surface. TEM shows multi-faceted AuNPs in the range of 20–30 nm. The reactivity of AuNPs/JPS for the transfer hydrogenation of nitroarene as well as hydrogenation of quinoline under molecular H₂ pressure was evaluated. Sodium borohydride, when used as the hydrogen source, demonstrates a high catalytic efficiency in the transfer hydrogenation reduction of 4-nitrophenol (4-NP). Quinoline is quantitatively and chemoselectively hydrogenated to 1,2,3,4-tetrahydroquinoline (py-THQ) using molecular hydrogen. Reusability studies show that AuNPs are stable on the support surface and their selectivity is not affected.     

Multiarm Star-Shaped Polydimethylsiloxanes with a Dendritic Branching Center

New multiarm stars have been synthesized based on polylithium derivatives of high-generation carbosilane dendrimers. In the synthesis of multiarm stars based on the eighth-generation dendrimer, steric hindrances were observed even during the synthesis of a polylithium initiator. Subsequently, this led to chain transfer reactions between growing arms, as well as other side effects. As a result, dense nanogel formations with a higher tendency of ordering than in classical objects of this type were isolated from the reaction mixture. The study of the rheology of multiarm stars based on sixth-generation dendrimers made it possible to determine the activation energies of viscous flow in these objects, which makes it possible to consider them as objects with a macromolecular nature and a reptation flow mechanism.