N-异丙基-O-芳基-O'-半乳吡喃基硫代磷酰胺酯的合成、结构及生物活性

报道了新型N-异丙基-O-芳基O''-半乳吡喃糖基硫代磷酰胺酯的合成,并对有关反应进行了讨论。通过重结晶分离得到了化合物N-异丙基-O-(对-氯苯基)-O''-半乳吡喃糖基硫代磷酰胺酯的纯异构体,单晶X射线衍射分析结果表明,此纯异构体分子中手性磷原子的构型为R.初步测定了这类化合物的除草活性及抗病活性。     

O－烷基，O－芳基硫代磷酰取代硫脲和O－烷基硫代磷酰－双－取代硫脲的研究（Ⅱ）

用硫氰酸钾与硫代磷酰氯制备了硫代磷酰异硫氰基酯和二异硫氰基酯，并以其与不同胺反应，合成了硫代磷酰取代硫脲和硫代磷酰－双－取代硫脲两系列２０个新的有机磷化合物，经~１ＨＮＭＲ、ＩＲ及元素分析确定了它们的化学结构，测定了它们的生物活性。结果表明只有Ｏ－异丙基，Ｏ－（４－甲基－２－硝基苯基）－Ｎ＇－萘基硫代磷酰硫脲（ＰＤ－１）具有较好的杀菌活性。     

O—乙基—N—异丙基（取代硫脲基）硫代磷酰胺酯类衍生物杀菌作用…

研究了一系列Ｏ－乙基－Ｎ－异丙基（取代硫脲基）硫代磷酰胺酯类化合物的杀菌活性，发现分子的活性中心在硫脲基上，其氮原子所连的取代基对活性有重要影响，采用取代基物理参数化合物对多种植物病菌的抑制活性，进行了结构与活性定量关系的研究，建立了较好的民性的盯关笥，预测出更高活性的化合物并得到实验证实。     

O—（1—甲硫基乙叉胺基）硫代磷酰胺（酯）的合成及生物活性…

首次报道了甲硫基乙醛肟与硫代磷酰氯的缩合反应，合成了１６种新型Ｏ－（１－甲硫基乙叉胺基）硫代磷酰胺酯及硫代磷酸酯类化合物，化合物６ｂ具有很好的杀虫活性。     

应用FTIR光谱研究不同取代苯胺对O－乙基－N－异丙基（取代硫脲基）硫代磷酰胺酯生成反应的影响

应用ＦＴＩＲ光谱研究不同取代苯胺对Ｏ－乙基－Ｎ－异丙基（取代硫脲基）硫代磷酰胺酯生成反应的影响何兰龄，赖城明，林，徐谨民，王永泰，杨华铮，吴烨（南开大学化学系，天津，３０００７１）（南开大学中心实验室）（南开大学元素有机化学研究所）关键词ＦＴＩＲ，取...     

2＇，3＇－O－异亚丙基－5＇－O－［N，N－二（2－氯乙基）磷酰胺基］核苷的合成

２＇，３＇－Ｏ－异亚丙基－５＇－Ｏ－［Ｎ，Ｎ－二（２－氯乙基）磷酰胺基］核苷的合成陈茹玉，迟国臣，陈小茹（南开大学元素有机化学研究所，天津，３０００７１）关键词核苷，亚磷酰化，抗肿瘤活性很多核苷类化合物具有很好的抗肿瘤、抗病毒等生物活性，某些化合物已...     

S—烯丙基—O—取代苯基硫代磷（膦）酸衍生物的合成及杀菌活？…

Ｏ,Ｏ－丙基硫代磷（膦）酸酯（６）与三氯氧磷发生异构化氯化反应得到Ｓ－烯丙基硫代磷（膦）酰氯７和Ｏ－烯丙基磷酰二氯酯（８）,７在碱性溶液中与取代酚反应,合成了１８个新的标题化合物,生物活性测试表明,这些化合物均有一定的杀菌活性,有些化合物还具有较好的杀菌活性或杀虫活性。     

硫代磷酰基硫脲与某些含氯双官能团试剂的成环反应

Ｏ－乙基－Ｎ－异丙基硫代磷酰硫脲衍生物与氯乙酰氯、二氯乙酰氯及三氯乙酰氯，在碱存在下可发生关环反应，得到相应的噻唑啉酮类衍生物，讨论了不同试剂及反应条件对产物结构的影响，而Ｏ－乙基－Ｎ－异丙基硫代磷酰硫脲与氯乙醛关环，则生成相应的噻唑衍生物，所有化合物经元素分析、＾１ＨＮＭＲ、ＩＲ及ＭＳ证实，其中部分化合物显示出一定的除草活性。     

S—烷基—O—多氯苯基硫代磷（膦）酸衍生物的合成及杀菌活性研究

Ｏ，Ｏ－二烷基硫代磷（膦）酸酯与三氯氧磷发生异构化氯化反应生成Ｓ－烷基硫代磷（膦）酰氯，后者在缚酸剂存在下与多氯酚反应得到标题化合物，此类化合物也可以用传统方法，从Ｓ－烷基硫代磷酰二氯先后与多氯酚及其它亲核试剂反应得到。对所合成的２８个新化合物的平碟试验表明，在０．００５％浓度下对小麦赤霉等１２种植物病菌均表现了明显的抑制活性。     

O—烷基苯基硫代磷酰取代硫脲的合成（Ⅲ）：含P—C键化合物的…

利用Ｏ－烷基苯基硫代磷酸酸异硫氰基酯与胺与胺的加成反应，合成了两系列Ｏ－烷基苯基硫代磷酰取代硫脲化合物，经元素分析、ＩＲ和＾１ＨＮＭＲ确定了它们的结构，并进行了除草活性的测试。     

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.     

Synthesis,characterization, and anticancer activity of some metal complexes with a new Schiff base ligand

A new Schiff base ligand, 2-((E)-((4-(((E)-benzylidene)amino)phenyl)imino)methyl)-naphthalene-1-ol, was prepared by the reflux condensation of p-phenylenediamine with 2-hydroxy-1-naphthaldehyde and benzaldehyde. Metal complexes were prepared by reacting the ligand with metal salts: VCl₃, CrCl₃·6H₂O, MnCl₂·3H₂O, FeCl₃·6H₂O, CoCl₃·6H₂O, NiCl₂·6H₂O, CuCl₂·2H₂O, and ZnCl₂. The ligand and its metallic complexes were characterized by various techniques such as elemental analysis, AAS, NMR, IR, UV–Vis, TGA, DTA, XRD and TEM. The data confirmed that the ligand coordinated with the metal ions in a bidentate nature, bonding through its azomethine nitrogen atom and phenolic oxygen atom; this gave an octahedral geometry. The XRD patterns of the complexes indicated that they were of various structures: the Mn(II), Co(III), and Cu(II) complexes were triclinic, the ligand and Ni(II) complex were orthorhombic, the V(III) and Zn(II) complexes were hexagonal, the Cu(II) complex was monoclinic, and the Fe(II) complex was cubic. TEM analysis confirmed that the complexes were nanoscale in nature. The antibacterial and antifungal activities of the ligand and its complexes against Salmonella enterica serovar typhi and Candida albicans were investigated by the hole plate diffusion method. It was observed that the Co(II) and Zn(II) complexes had intermediate antibacterial activities, while the V(III) complex had the highest activity against C. albicans fungi. The in vitro anticancer activities of the ligand and its metal complexes were tested towards PC-3, SKOV3, and HeLa tumour cell lines, where they exhibited higher antitumour activities against these selected human cell lines than clinically used drugs such as cisplatin, estramustine, and etoposide.     

新型香豆素类白藜芦醇衍生物的合成及其生物活性研究

白藜芦醇是一种具有广泛生物活性的茋类化合物。为了寻找活性较强的新型分子,以白藜芦醇为原料出发,经Vilsmeier甲酰化和Knoevenagel缩合,合成了3个未见文献报道的香豆素类白藜芦醇衍生物 (E)-7-羟基-5-(4-羟基苯乙烯基)香豆素（3a-3c）,其结构经1H NMR、13C NMR和HRMS确证。抗炎和抗氧化活性结果发现,化合物3a具有与地塞米松相当的抗炎活性,并对超氧阴离子和羟基自由基有较强的清除作用,可做进一步研究。     

N-苄氧/烷氧苯基-4,6-二取代嘧啶胺类化合物的合成、晶体结构及除草活性

以5种苄氧基/烷氧基苯胺为基础, 设计合成了系列新颖的N-苄氧/烷氧苯基-4,6-二取代嘧啶胺类化合物, 其结构经1H NMR、MS及元素分析确证, 其中化合物5r的单晶结构经X射线单晶衍射分析确证. 油菜平皿法和稗草小杯法测试除草活性结果表明, 4种苄氧基/烷氧基苯胺3a, 3b, 3d, 3e具有较好的除草活性, 在100 μg/mL浓度下对单子叶稗草生长抑制率可达到77.3%—88.5%. KARI活性测试结果表明, 化合物5a—5s有较弱的KARI抑制活性.     

Syntheses and Biological Activities of Novel 3-Bromo-1-（3-chloropy- ridin-2-yl）-N-hydroxy-N-aryl- 1H-pyrazole-5-carboxamides

A series of novel 3-bromo-1-（3-chloropyridin-2-yl）-N-hydroxy-N-aryl-lH-pyrazole-5-carboxamides was synthesized by the reaction of pyrazole carbonyl chloride with each of substituted phenylhydroxyamines. The latter ones were prepared in good yields by reducing substituted nitrobenzene compounds with Zn/NH4CI reductant system in alcohol. Structures of the title compounds were determined by IR, 1H NMR, and HRMS. Their insecticidal and fungicidal activities were evaluated by larvicidal test against oriental armyworm and the mycelium growth rate method, respectively.     

Synthesis,antimicrobial and anti-inflammatory activities of some novel 5-substituted imidazolone analogs

In view of potent antimicrobial and anti-inflammatory activities exhibited by 5-substituted imidazolones, a variety of novel imidazolone analogs 3a-l were synthesized by the condensation of different substituted oxazolones 1 with various aromatic amines 2. All the synthesized compounds were screened for in vitro activities against a panel of Gram-positive and Gram-negative bacteria and the yeast-like pathogenic fungus Candida albicans. Several analogs produced good or moderate activities particularly against the tested Gram-positive bacteria Micrococcus luteus and Gram-negative bacteria Pseudomonas aeruginosa and. Meanwhile, compounds 3b and 3c displayed marked antifungal activity against C. albicans. In addition, the in vivo anti-inflammatory activity of the synthesized compounds was determined using the carrageenin-induced paw oedema method in rats. Two of 5-substituted imidazolone derivatives, 3k and 3d show good anti-inflammatory activity. The structures of all the newly synthesized compounds were elucidated using IR, ¹H NMR and ¹³C NMR.     

Synthesis, Structure and Antitumor Activities of Tridccapeptide PSPP3 from Papaver Somniferum Pollen

Pollenplaysakeyroleinthereproductiveprocessofhigherplant,whichcontainsmuchimportantsubstancewithdifferentphysiologicalactivities,ofwhichpeptideandproteinareimportantonesl'2.Pollenisstillwidelyusedasnutritiveandhealthfulfoodinmanycountriesl.Inrecentyears,wehavepaidmuchattentiontothestudiesontheisolation,structurecharacterizationandsynthesisofsomeoligopeptidesfromseveralkindsofpollens'-',andfoundthattheyhadsomeactivitiesofpromotingimmunityandrestrainingsomecancercelldivisions-7.Inpreviousstudies…     

Synthesis and Biological Evaluation of Novel Anthranilic Diamides Containing N-H/CH3-1H-Pyrazole

In order to systematically study the structure-activity relationship of anthranilic diamides and develop insecticides with simple structure and high efficiency, a series of novel anthranilic diamides containing N-H/CH₃-1H-pyrazole was designed and synthesized. Their chemical structures were characterized by ¹H NMR spectra, high resolution mass spectrometry(HRMS) or ¹³C NMR spectra. The preliminary bioassay results indicated that all title compounds displayed moderate insecticidal activity against oriental armyworm(Mythimna separata) at 200 mg/L and fungicidal activities against six kinds of fungi at 50 mg/L, especially compound 5i showed 50% insecticidal activity at 25 mg/L. In addition, some compounds exhibited certain antitumor activities. It was demonstrated that the introduction of CH₃ group into pyrazole ring was superior to H for the insecticidal activity.     

黑果枸杞叶多糖LRLP3的结构、抗氧化活性及免疫活性

黑果枸杞叶经水提醇沉, 离子交换柱层析和凝胶柱层析分离纯化, 得到平均分子量为79400的均一多糖组分LRLP3. 对该多糖的理化性质、 结构、 抗氧化活性及免疫活性的研究结果表明, LRLP3为多分支结构, 主链为(1→3)βGalp, 大部分半乳糖6位存在分支; 支链由(1→6)βGalp, (1→4)βGalp, (1→3)βAraf, (1→3)αArap, (1→5)βAraf和(1→2,4)αRhap组成, 非还原末端由αAraf, βGalp和βGlcp组成. LRLP3具有较强的还原能力, 可显著清除1,1-二苯基-2-三硝基苯肼(DPPH)自由基、 羟自由基和超氧阴离子自由基, 有效抑制Cu²⁺/H₂O₂诱导的蛋白氧化损伤和H₂O₂诱导的细胞氧化损伤. LRLP3在体外对未经诱导和经刀豆蛋白(ConA)或脂多糖(LPS)诱导的小鼠脾细胞增殖均有促进作用.