N-[5-(1-邻(对)氯苯氧乙基)-1,3,4-噻二唑-2-基]-N'-芳酰基硫脲的合成与生物活性

为了寻找高活性的杂环农药,通过2-氨基-5-(1-邻氯苯氧乙基)-1,3,4-噻二唑和2-氨基-5-(1-对氯苯氧乙基)-1,3,4-噻二唑与芳酰基异硫氰酸酯反应,合成了26种新的芳酰基硫脲.采用核磁共振氢谱、红外光谱及元素分析确证了它们的结构.初步的生物活性测定试验表明,部分目标化合物表现出良好的植物生长调节活性,其中3c,3d,3e,4b和4c具有优良的生长素活性.     

N-(5-对溴苯氧甲基-1,3,4-噻二唑-2-基)-N′-芳氧乙酰基硫脲的合成与生物活性

2-氨基-5-对溴苯氧甲基-1,3,4-噻二唑与芳氧乙酰基异硫氰酸酯反应,合成了9种新的芳氧乙酰基硫脲。其结构经1H NMR,IR和元素分析确证。初步的生物活性实验结果表明,部分化合物具有较好的植物生长调节活性。     

Synthesis and Antimicrobial Activities of Some Heterocyclic Systems from 2-Furoyl Isothiocyanate

2-Furoyl isothiocyanate (1) is used as a building block in synthesizing different heterocyclic systems of anticipated biological activities. Thus, isothiocyanate 1 was reacted with different nucleophilic reagents to produce five- and six-membered heterocyclic systems such as 1,2,4-triazoline, thiadiazolidine, quinazoline, benzothiazole, benzoxazole, benzimidazole, thiazolidine, and imidazolidine. The structures of all the synthesized compounds were confirmed by microanalytical and spectral data. The antimicrobial activity of some of the synthesized compounds was tested.

Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file.     

N-取代吡唑亚甲胺基-N＇-取代苯基(硫)脲的合成

硫脲;生物活性;N-取代吡唑亚甲胺基-N＇-取代苯基(硫)脲的合成     

1-芳基-3-(3-(4-氧香豆素基)苯基)硫脲衍生物的合成及抑菌活性

为了筛选出具有较高抑菌活性的含香豆素的硫脲类衍生物,本文以4-羟基香豆素为原料,经氯化、醚化、异硫氰酸化和加成反应合成了一系列1-芳基-3-(3-(4-氧香豆素基)苯基)硫脲衍生物,其结构经红外光谱(IR)、核磁共振谱(NMR)和质谱(MS)等技术手段进行了表征。结果表明,目标化合物对水稻白叶枯菌和柑橘溃疡菌均具有较好的抑制活性。其中化合物4k、4l、4m和4n抑制水稻白叶枯菌活性EC_(50)值分别为137.42、131.05、129.23和117.43 mg/L,优于对照药剂噻菌铜的活性(195.24 mg/L);化合物4k、4l、4m和4n抑制柑橘溃疡菌活性EC_(50)值分别为97.02、94.31、102.28和90.52 mg/L,优于噻菌铜的活性(120.25 mg/L)。     

N-(5-对三氟甲基苯基-1,3,4-噻二唑-2-基)-N′-芳酰基硫脲的合成及生物活性

用2-氨基-5-对三氟甲基苯基-1,3,4-噻二唑与芳酰基异硫氰酸酯反应,合成了14种新的标题化合物(3a~3n),其的结构经1H NMR,IR和元素分析确证。室内初步的生物活性测定试验表明,部分标题化合物具有良好的植物生长调节活性,其中3e,3g和3m的生长素活性更好。     

Synthesis and Structure Characterization of Novel Triazole Compounds Containing 1,3-Dioxolane

Five novel triazole compounds containing group 1,3-dioxolane were designed and synthesized by taking difenoconazole as the start compound and changing diphenyl ether for benzyl phenyl ether. Their structure swere confirmed by elemental analyses, ^1H NMR and IR spectra. The single crystal structure of 2-[-4-(2,4-dichlorophenylmethoxy] phenyl-2-(1,2,4-triazol-l-yl ) methane-I, 3-dioxolane was determined by means of X-ray diffraction. The preliminary bioassays showed that the synthesized compounds exhibited some activities of fungicides and plant growth regulators.     

Synthesis, antibacterial and antifungal activity of some derivatives of 2-phenyl-chromen-4-one

Some derivatives of 2-phenyl-chromen-4-one (flavone ring) have been synthesized and tested for antibacterial and antifungal activities along with their chalcone precursors against four human pathogenic bacteria and five plant mould fungi. The structures of the synthesized compounds were elucidated by UV, IR and¹H NMR spectroscopic techniques, and elemental analysis. The antibacterial and antifungal screens of the synthesized compounds were performed in vitro by the filter paper disc diffusion method and the poisoned food technique.     

含三唑二硫代膦酸酯及硫代(或二硫代)磷酰胺酯类衍生物的研究

近年来,分子中含有1,2,4-三唑的非有机磷化合物作为杀菌剂和植物生长调节剂已受到广泛重视.为进一步开发有机磷和三唑类农药新品种,科学工作者合成了含三唑的有机磷化合物,发现某些化合物对植物的白粉病及锈病具有较强的生理活性,故进一步合成和研究各类新型含三唑的有机磷化合物具有较大的意义。作者曾报道某些含三唑的二硫代磷酸酯类化合物的合成及生物活性,发现某些化合物具有一定的杀菌、除草及调节植物生长作用.     

含1,3-二氧戊环的新三唑类化合物的结构表征及生物活性研究

根据生物电子等排理论合成了7种含1,3-二氧戊环的新三唑类化合物。其结构通过元素分析、核磁共振氢谱、红外光谱、质谱和单晶X射线衍射法确证。采用离体平皿法对它们的杀菌活性进行了比较，同时测定了它们的植物生长调节活性。测定结果表明化合物4a对黄瓜子叶生根具有较强的促进作用，促进率达159％。     

Studies on Synthesis and Biological Activities of Novel Triazole Compounds Containing Pyrimidine or N,N-Dialkyldithiocarbamate Ring

IntroductionAs an important type of fungicides,triazolecompounds are highly efficient,low poisonous andinward absorbents[1— 4] .At present,the studies ontriazole derivatives have mainly been concentratedon the compounds with triazole group as the onlyactive group.The report of triazloe compoundsthat contain both a triazole group and other activegroups in a single molecule has rarely been found.Some pyrimidines have been used as high efficientand low poisonous fungicides[5] in control of pow-d…     

N-取代芳酰氨基-5-氟代苯基-2-呋喃甲酰硫脲的合成与生物活性测定

从5-氟代苯基-2-呋喃甲酸出发, 经酰化、异硫氰酸酯化, 再与取代芳酰肼反应合成了20个未见文献报道的N-取代芳酰氨基-5-氟代苯基-2-呋喃甲酰硫脲. 目标产物的结构经IR, ¹H NMR和元素分析测定确证. 初步生物活性测试表明, 部分化合物对棉花枯萎病、黄瓜灰霉病、苹果轮纹病和棉花炭疽病有较好的选择性杀菌活性; 部分目标化合物有较好的除草活性.     

一类新型多取代嘌呤类化合物的合成及生物活性

以4-氯-5硝基嘧啶(3)为起始物, 经胺解、还原和环合等反应, 构建了新型的多取代嘌呤-8-硫酮(6)结构. 通过化合物6与卤代物的反应, 获得了该杂环的8位巯基衍生物7a-1~7, 7b-1~5和8, 其结构经元素分析, 1H NMR, IR及MS确证. 生物活性测试结果表明,  化合物6和7具有一定的除草和抗烟草花叶病毒活性.     

四氢咪唑并[2',1':2,3]噻吩并[5,4-c]哌啶衍生物的合成及抗肿瘤活性

以4-哌啶酮为原料,经过胺基保护、缩合、环合、脱保护等步骤,设计合成了一系列新型的5,6,7,8-四氢咪唑并[2',1':2-3]噻吩并[5,4-c]哌啶类化合物。通过核磁共振波谱仪(~1H NMR、~(13)C NMR)、质谱(MS)和元素分析确证了其结构。对其体外活性研究发现,该类化合物对乳腺癌细胞MCF-7具有一定的抑制活性,其中化合物5a的抑制活性最为显著,半数抑制浓度(IC_(50))值达到了8.6μmol/L。为此类化合物的抗肿瘤活性研究提供了参考。     

Overview on the recently developed thiazolyl heterocycles as useful therapeutic agents

Thiazoles are important heterocyclic compounds which have many biological activities and different applications such as useful ligands, in optical sensors, etc. A literature survey shows that there are different routes to thiazoles. One of the most frequently used synthetic approaches consists of a reaction between α-halocarbonyl compounds with a CSNH₂ moiety. In this mini-review we have classified the contents based on the reagent or material providing the sulfur atom of the thiazole ring. Also, among many articles which have been devoted to thiazole syntheses here we presented some synthetic approaches published from 2012 to 2014.     

The immobilized Ni(II)‐thiourea complex on silica‐layered copper ferrite: A novel and reusable nanocatalyst for one‐pot reductive‐acetylation of nitroarenes

In this study, magnetically nanoparticles of CuFe₂O₄@SiO₂@PTMS@Tu@Ni(II) as novel and reusable catalyst were prepared. Synthesis of the Ni (II)‐nanocatalyst was carried out through the complexation of Ni(OAc)₂·4H₂O with the immobilized thiourea on silica‐layered CuFe₂O₄. The prepared nanocomposite system was then characterized using SEM, EDX, XRD, VSM, ICP‐OES, Raman, UV–Vis and FT‐IR analyses. Catalytic activity of the Ni(II)‐CuFe₂O₄ system was investigated towards rapid reduction of aromatic nitro compounds to arylamines with sodium borohydride as well as one‐pot reductive‐acetylation of nitroarenes to acetanilides with NaBH₄/Ac₂O system without the isolation of intermediate arylamines. All reactions were carried out in H₂O within 3–7 min to afford the products arylamines/acetanilides in high to excellent yields. Reusability of the Ni(II)‐nanocatalyst was examined for seven consecutive cycles without the significant loss of the catalytic activity.     

4-羟基-2-吡啶酮类化合物的合成研究进展

4-羟基-2-吡啶酮是天然生物碱结构母核,同时也是一类重要的医药中间体,该类衍生物具有抗真菌、抗菌和抗肿瘤等多种生物活性.因此,其合成得到了广泛的研究和关注.综述了近年来4-羟基-2-吡啶酮类化合物的合成方法及其研究进展.     

Identification of active compounds from medicinal plant extracts using gas chromatography-mass spectrometry and multivariate data analysis

Conventional methods of drug discovery from natural products include bioassay-guided fractionation, which is tedious and has low efficiency. The aim of this work is to develop a platform method to rapidly identify bioactive compounds from crude plant extracts and their partially purified fractions using multivariate data analysis (MVDA). Soxhlet extraction and liquid-liquid fractionation were used to prepare different extracts and fractions from the leaves of a medicinal plant, Ardisia elliptica. The extracts and fractions were analysed chemically using GC-MS, and their ability to inhibit platelet aggregation was investigated. Two MVDA methods were developed and optimised to analyse the results. In the first method, compounds with the highest contribution scores for biological activity calculated by different models were listed as potential antiplatelet compounds. For the second MVDA method, a correlation of the concentrations of constituents and biological activities in the various extracts and fractions for each compound was done. Compounds with the highest correlation coefficients were identified as potential antiplatelet compounds. One of the predicted components was isolated, purified and confirmed to possess antiplatelet effects. This platform method can be developed and optimised for other plant extracts and biological activities, thus reducing time and cost of drug discovery while improving efficiency.     

N-[5-(1-邻(对)氯苯氧乙基)-1,3,4-噻二唑-2-基]-N'-芳酰基硫脲的合成与生物活性

为了寻找高活性的杂环农药, 通过2-氨基-5-(1-邻氯苯氧乙基)-1,3,4-噻二唑和2-氨基-5-(1-对氯苯氧乙基)-1,3,4-噻二唑与芳酰基异硫氰酸酯反应, 合成了26种新的芳酰基硫脲. 采用核磁共振氢谱、红外光谱及元素分析确证了它们的结构. 初步的生物活性测定试验表明, 部分目标化合物表现出良好的植物生长调节活性, 其中3c, 3d, 3e, 4b和4c具有优良的生长素活性.     

N-(2-羧基-1,3,4-噻二唑-5-基)-N''-芳酰基硫脲与芳氧乙酰基硫脲的合成与生物活性

为了寻找高活性的杂环农药,用5-氨基-1,3,4-噻二唑-2-羧酸与芳酰基异硫氰酸酯及芳氧乙酰基异硫氰酸酯反应,合成出18种新的芳酰基硫脲与芳氧乙酰基硫脲,采用红外光谱、核磁共振氢谱和元素分析证明了其结构,初步的生物活性测定试验表明,部分目标化合物具有良好的植物生长调节活性,其中2c,2d,3b和3g具有良好的生长素活性.