活性聚合,表现活性聚合和准活性聚合

活性聚合是连锁聚合反应体系中链转移和终止反应速率为零时的特殊反应类型，表现活性聚合和准活性聚合则是链转移或终止反应未被完全消除而人有活性聚合物特征两类聚合物反应，是非活性聚合活性聚合过渡和逼近时的两种聚合反应类型，本文对活性聚合，表现活性聚合和准活性聚合的基本概念及它们之间的区别作了简单的介绍。     

活性聚合、表观活性聚合和准活性聚合

活性聚合是连锁聚合反应体系中链转移和终止反应速率为零时的特殊反应类型，表现活性聚合和准活性聚合则是链转移或终止反应未被完全消除而又具有活性聚合特征的两类聚合反应，是非活性聚合向活性聚合过渡和逼近时的两种聚合反应类型。本文对活性聚合、表观活性聚合和准活性聚合的基本概念及它们之间的区别作了简单的介绍。     

1,2,4-三唑类化合物的合成及其农用活性研究进展

1,2,4-三唑类化合物是生物活性分子的重要结构单元,具有多种药理活性,特别是在抗真菌、杀虫和除草等农用活性方面得到广泛应用。本文对部分1,2,4-三唑环上的活性位点改性研究及其在农用活性方面的应用进行了总结归纳,期望为后期该类化合物的设计合成及农用活性研究提供参考和借鉴。     

具有生物（理）活性的二茂铁衍生物

结合作者的研究工作，本文对具有生物（理）活性的二茂铁衍生物进行了综述，探讨了生物（理）活性与结构之间的相互关系。     

活性点数对煤焦气化反应的影响：I.气化活性的评价

在活性点评价装置上，以二氧化碳与煤焦进行气化反应，测得了高温时煤焦的活性点数，实验发现其活性点数随煤种而变。煤化程度低的煤种具有较多的活性点数，随煤化程度的提高。活性点数相应减少，气化反应速率与活性点数成线性关系，不同煤种的气化速率的数十倍差别是由于煤焦具有的活性点数的差异所致。活性点数是表征煤焦气化活性的一种重要标准。     

具有农药活性的微生物源核苷类化合物

微生物天然产物在新农药的研究与开发中占据着重要的地位。核苷作为一类重要的生理活性物质, 具有丰富多样的结构及生物活性。本文对微生物来源的具有农药活性的核苷类化合物进行总结,重点综述了具有农药活性的微生物源嘧啶或嘌呤、核苷及其衍生物及核苷酸类似物等三类微生物源核苷类化合物,分别对其来源、结构多样性、农药活性及杀虫、杀菌及抗病毒作用机制进行了概括, 以期对新型农用抗生素的开发及新农药创制提供一些有益的借鉴。     

含1,2,4-三唑环的亚胺及酰亚胺类化合物的合成及生物活性

以取代苯甲酸为原料,经酯化、肼解、成盐和环化反应得到关键中间体4-氨基-3-芳基-1,2,4-三唑-5-硫酮,再分别与芳醛和邻苯二甲酸酐缩合得到亚胺及酰亚胺,最后经硫醚化反应合成了24个新型的含有1,2,4-三唑结构单元的亚胺及酰亚胺类化合物,其结构经质谱、红外光谱、核磁共振及元素分析确认.初步生物活性测试结果表明,在实验浓度下大部分化合物表现出一定的杀菌活性,尤其是化合物9a,9d和9e对水稻纹枯病菌的抑制活性与对照杀菌剂氟硅唑相当.初步的细胞毒性实验结果表明,化合物7c,7f和9k对人肺癌细胞(A549)的抑制活性与对照药品5-氟尿嘧啶基本处于同一水平.     

离子型有机锡化合物的合成及其生物活性

利用有机锡卤化物与有机酸在有机胺存在下反应合成了一系列离子型有机锡化合物,分子通式为[HNR3][(PhCH2)3Sn(μ2-SCH2COO)Cl]、[HNR3][Ph3Sn)3(O2CCH2CO2)2]·CH3CH2OH和[HNR3] [MeCy2ClSnO2CCH2CO2SnClCy2Me]。化合物的体外抗肿瘤、杀菌和杀螨活性测试结果表明,部分化合物具有很好的生物活性。[HNR3][(Ph3Sn)3(O2CCH2CO2)2]·CH3CH2OH和[HNR3] [MeCy2ClSnO2CCH2CO2SnClCy2Me]配合物对人肺癌细胞株A-549、结肠癌细胞株HCT-8和肝癌细胞株Bel-7402的抑制率约为90%,[HNR3][MeCy2ClSnO2CCH2CO2SnClCy2Me]配合物对小麦赤霉、番茄早疫、芦笋茎枯、苹果轮纹、花生褐斑的杀死率都为100%,配合物[HNR3] [MeCy2ClSnO2CCH2CO2SnClCy2Me]的杀螨活性致死率大于90%。     

Synthesis and Antioxidant Activity of Sapriparaquinone Analogues

It has been considered that the lipid peroxidition damage was involved in aging and pathological disorders. Some phases of atherosclerosis, neuronal ceroid lipofuscinosis, intermittent claudication, oxygen toxicity, and liver injury caused by orotic acid, ethanol, phosphorous or chlorinated hydrocarbons have been discussed in relation to lipid peroxidion1-3. We found that a series of unique 4,5-secoditerpenoidal compounds isolated from the medicinal plant Salvia prionitis showed various bioact…     

活性点数对煤焦气化反应的影响Ⅰ．气化活性的评价

在活性点评价装置上，以二氧化碳与煤焦进行气化反应，测得了高温时煤焦的活性点数。实验发现其活性点数随煤种而变。煤化程度低的煤种具有较多的活性点数，随煤化程度的提高，活性点数相应减少。气化反应速率与活性点数成线性关系，不同煤种的气化速率的数十倍差别是由于煤焦具有的活性点数的差异所致。活性点数是表征煤焦气化活性的一种重要标准。     

取代嘧啶化合物的合成和生物活性研究

合成了14个新型取代嘧啶类化合物,结构经质谱、红外光谱、氢核磁共振光谱和元素分析确证.杀虫、杀菌和除草活性测定结果表明,部分化合物具有良好的杀菌活性.在嘧啶环的2-位上导入二甲氨基时表现出杀菌活性,但在嘧啶环的5-位上有甲基取代基时,杀菌活性下降.在嘧啶的4-位导入苯氧基时,显示出良好的杀菌活性,如化合物3b,3c和3e,苯环上的最优取代基是2-硝基-4-三氟甲基.     

Antifungal,anti-inflamatory and neuritogenic activity of newly-isolated compounds from Disporopsis aspersa

Abstract

A new ester (1) and a terpenoid (2) were isolated from the dried whole plant of Disporopsis aspersa (H_UA) E_NGL. ex D_IELS for the first time and their structures were elucidated, as well as their biological activities are described. The two compounds all showed good antifungal activities, especially furanone (2) exhibited better antifungal activity against Pseudoperonospora cubensis and Phytophthora infestans with EC₅₀ value of 22.82, 18.90?μg/mL, respectively. Compound 1 exhibited a significant promotion on the neurite outgrowth in NGF-induced PC-12 cells, and moderate inhibition on the NO production induced by lipopolysaccharide (LPS) in BV-2 microglial cells.     

Synthesis and Antimicrobial Activity of Substituted Phenophosphazines

Several Schiff base derivatives of phenophosphazines were synthesized by the reaction of amino phenophosphazines and aromatic aldehydes in equimolar ratio, using methanol as solvent. Possible structures have been proposed on the basis of elemental analysis, IR, and ¹H NMR spectral studies. The antibacterial and antifungal activities of the above mentioned Schiff base derivatives have been evaluated against pathogens E. coli, S. typhi, S. aureus, B. subtilis, A. niger, and C. Albicans.     

Microbiological and Antioxidant Activity of Phenolic Compounds in Olive Leaf Extract

According to many reports, phenolic compounds isolated from olive leaves have very good biological activities, especially antimicrobial. Presently, the resistance of microorganisms to antibiotics is greater than ever. Therefore, there are numerous recent papers about alternative solutions for inhibiting their influence on human health. Olive leaf is studied as an important source of antimicrobials with low cost and used in medicine. Numerous publications on involving green technologies for isolation of active compounds from olive leaves have appeared over the past few decades. The present review reports on current knowledge of the most isolated phenolic compounds from olive leaf extract as well as methods for their isolation and characterization. This paper uses recent research findings with a wide range of study models to describe the antimicrobial potential of phenolic compounds. It also describes the vast range of information about methods for determination of antimicrobial potential focusing on effects on different microbes. Additionally, it serves to highlight the role of olive leaf extract as an antioxidants and presents methods for determination of antioxidant potential. Furthermore, it provides an overview of presence of enzymes. The significance of olive leaves as industrial and agricultural waste is emphasized by means of explaining their availability, therapeutic and nutritional effects, and research conducted on this field.     

Synthesis of new triphenodithiazine- and indolocarbazolediones of biological interest

Tetrabromo-p-benzoquinone reacted with excess aromatic amines to give 2,5-dirylamino-3,6-dibromo-p-benzoquinones. The latter molecules on heating with sodium sulfide in alcohol in the presence of air gave triphenodithiazinediones. Heating with copper powder in nitrobenzene transformed these compounds into the respective indolocarbazolediones. Comparative antimicrobial and antifungal activities of the studied compounds were determined and discussed.     

Antituberculosis,antifungal and thermal activity of mixed ligand transition metal complexes

Mixed‐ligand complexes of the type [M(CQ)(Ph)(OH)(H₂O)], where M = Cu(II), Ni(II), Co(II) and Mn(II), have been investigated. Furthermore, there has been some additional work investigating the effect of metal ions on biological activity. Aiming to obtain novel transition metal complexes that exhibit biological activity, we have synthesized mixed ligand complexes using clioquinol (5‐chloro‐7‐iodo‐8‐hydroxyquinoline) and 1,10‐phenanthroline as ligands. The compounds were characterized using IR, FAB mass spectroscopy, elemental analyses, electronic spectra, magnetic measurements and gravimetric analyses. The kinetic parameters such as order of reaction, the energy of activation, the pre‐exponential factor, activation entropy, activation enthalpy and free energy of activation have been reported. The complexes show antituberculosis and antifungal (minimal inhibitory concentration) activities. Copyright © 2010 John Wiley & Sons, Ltd.     

In vitro biological activities and preliminary phytochemical screening of different extracts from Achillea sintenisii Hub- Mor

This study was designed to investigate in vitro biological activities and phytochemical composition of aqueous and ethanolic extracts from Achillea sintenisii Hub- Mor. (AS). To determine the chemical composition of AS extracts, phytochemical analyses were performed by using HPLC–ESI-Q-TOF-MS-MS. Afterwards, both extracts were investigated in terms of their effect on fibroblast proliferation, collagen synthesis, and hydrogen peroxide-induced damage. In addition to cell culture analysis, antibacterial, antioxidant, hyaluronidase inhibitory activities and total phenolic contents of the extracts were analyzed in cell-free systems. Our results demonstrated that the aqueous and ethanolic extracts did not show cytotoxic activity on fibroblasts, on the contrary, promoted fibroblast proliferation. Both AS extracts potently inhibited hyaluronidase activity and the inhibitory effect of ethanolic extract was comparable with the positive control, especially at high concentrations. The aqueous extract was the potent stimulator of collagen synthesis at 200 µg/mL concentration. Although the ethanolic extract showed antibacterial activity against all gram-positive bacteria, the aqueous extract was only effective against K. pneumoniae and B. subtilis. The ability of AS extracts, which have a rich phenolic compound content (≥50 mg GAE/g), to scavenge free radicals and protect fibroblasts against hydrogen peroxide-induced damage can be considered as a result of their antioxidant potential. Our findings scientifically support the widespread use of this plant, by demonstrating the pharmacological properties of the extracts.     

Fluorinated nucleosides: Synthesis and biological implication

A number of important pharmaceuticals have been discovered and developed based on fluorinated analogs of biologically active nucleosides. The introduction of fluorine into a nucleoside structure at an appropriate position has modulated and/or improved the pharmacological properties of a molecule. The present review deals with the synthetic methodology, structural and biological implication of carbohydrate-modified fluoronucleosides.     

Synthesis and Evaluation of the Tetracyclic Ring-System of Isocryptolepine and Regioisomers for Antimalarial,Antiproliferative and Antimicrobial Activities

A series of novel quinoline-based tetracyclic ring-systems were synthesized and evaluated in vitro for their antiplasmodial, antiproliferative and antimicrobial activities. The novel hydroiodide salts 10 and 21 showed the most promising antiplasmodial inhibition, with compound 10 displaying higher selectivity than the employed standards. The antiproliferative assay revealed novel pyridophenanthridine 4b to be significantly more active against human prostate cancer (IC₅₀ = 24 nM) than Puromycin (IC₅₀ = 270 nM) and Doxorubicin (IC₅₀ = 830 nM), which are used for clinical treatment. Pyridocarbazoles 9 was also moderately effective against all the employed cancer cell lines and moreover showed excellent biofilm inhibition (9a: MBIC = 100 µM; 9b: MBIC = 100 µM).     

Antifungal and cytotoxic substances from the stem barks of Desmos chinensis

Isounonal-7-methyl ether（1） and chinendihydrochalcone（2） together with 8 known compounds were isolated from the stem barks of Desmos chinensis.Their structures were determined on the basis of spectroscopic data.Compound 2 exhibited cytotoxic activity against MOLT-3 cancer cell line(IC₅₀ 7.16μg/mL) and antifungal activity against Pyricularia oryzae and Rhizoctonia solani with MIC values of 15.6 and 31.2μg/mL,respectively.