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In order to find active pesticide leading compounds, thinking about that triazolothiadiazoles had various biological activities, this paper designed and synthesized 11 novel title compounds from 3-substituted-4-amino-5-mercapto-1,2,4-triazoles with heterocyclic carboxylic acid via cyclization in the presence of phosphoryl chloride by the princple of combination of active strucural moieties. The structures of the title compounds were characterized by melting point, IR, 1HNMR and elemental analysis.

为了寻找高活性农药先导化合物,考虑到三唑并噻二唑衍生物具有广泛的生物活性,本文利用活性亚结构拼接原理,将活性基团分别引入1,2,4-均三唑并[3,4-b]-1,3,4-噻二唑杂环的3位和6位,合成了未见文献报道的3,6-二取代均三唑并[3,4-b]-1,3,4-噻二唑类化合物11个,并用IR、1HNMR及元素分析测试技术对其进行了结构表征。

In this study, new benzo[l,2,3]thiadiazole derivatives were designed according to relationship of structure and efficacy. The 9 novel compounds were synsthesized with following reactions. The chlorine atom in 2-chloro-3,5-dinitro-benzoic acid as beginning raw material was substituted by 2-methylpropane-2-thiol, esterified then with bromoethane, reduced by iron powder and cyclized to obtain ethyl benzo[l,2,3]thiadiazole-7 after diazonation reation.

本论文根据苯并噻二唑诱导剂的构效关系设计了新的苯并噻二唑的结构,并合成了9个未见文献报道的化合物,合成步骤如下:采用2-氯-3,5-二硝基苯甲酸为起始原料,苯环上的氯原子被叔丁基硫醇置换,羧酸由溴乙烷酯化,硝基由铁粉还原,随后经重氮化关环生成苯并[1,2,3]噻二唑-7-羧酸乙酯。

The best of them were 4c and 8d which exhibited 87% and 89% inhibition of Penicilium digitatum . And benzothieno[3,2-d]imidazol[1,2-a]pyrimidin-2,5(1H, 3H)-diones or benzothieno[3,2-d][1,2,4]triazol[1,5-a]pyrimidin-10(3H)-one only exhibited moderate inhibition.

而苯并噻吩并[3,2-d]嘧啶-4(3H)-酮和苯并噻吩并[3,2-d]咪唑并[1,2-a]嘧啶-2,5(1H,3H)-二酮以及苯并噻吩并[3,2-d][1,2,4]三唑[1,5-a]嘧啶-10(3H)-酮衍生物以及三唑醇衍生物均只表现出中等的抑制率。

Out-of-body experience certified curcumine could suppress the hyperplasy of the mice splenic lymphocyte.

方法通过噻唑蓝比色法比较姜黄素3种给药途径对小鼠脾淋巴细胞增殖的影响。

Methods: the chondrocytes of the rabbit condylar were derived from rabbit,and were cultured to the second generation in vitro,then hgfcdna transfected the cells.the capacity of cell proliferation was tested by mtt,the deferences of the type ii collagen were tested by sabc immunohistochemical of the type ii collagen after infected;the mrna levels were tested nd so on the mrna levels were tested by in situ hybridization of the type ii collagen between the transfection group and comparison group .

取兔膝关节软骨细胞体外培养至第二代,hgfcdna转染软骨细胞,空白质粒组为对照组;噻唑蓝检测软骨细胞的增殖能力,sabc免疫组化及原位杂交法测其ii型胶原在转染前后的变化与mrna的表达。

The proliferation of cells were detected by trypan blue exclusion, methyl thiazolyl tetrazolium assay, Hoechst33342 fluorescence staining and flow cytometry method.

利用台盼兰排斥试验、噻唑蓝比色法、Hoechst33342 荧光染色、流式细胞术测细胞周期法等实验技术分别检测了不同浓度AA 和DHA 对大鼠前体脂肪细胞活力、细胞周期及凋亡的影响。

We employed a cell line of mouse podocytes immortalized with the simian virus 40 large tumor antigen gene, and examined the cell proliferation using colony-forming and MTT assays following treatment with various concentrations of bFGF. BMP-7, alpha-smooth muscle actin e podocytes were detected by western blot. Methyl blue staining was used for the observation of cell morphology.

利用SV40肿瘤抗原转染所获得的永生性小鼠足细胞系培养,以集落形成法和噻唑蓝MTT还原实验测定不同浓度bFGF刺激下的足细胞增殖,采用SDS-聚丙烯酰胺凝胶电泳和Western blotting 检测BMP-7、alpha-平滑肌肌动蛋白、以及波形蛋白的蛋白质水平表达,同时以甲基兰染色观察细胞形态。

All the resulted products and key intermediates were characterized with EI-MS, 1H-NMR and 13C-NMR. The combined overall yield of these two compounds was up to 52%. The optimized reaction process is mild, easy to manipulate and control.

通过电子轰击质谱、核磁共振氢谱和碳谱对其产物及关键中间体的结构进行表征。2种含有不饱和侧链异噻唑类化合物的总收率达52%,优化后的合成路线条件温和,操作简单,易于控制。

According to the experience of the research of the indoles alkaloid, we designed a series of novel compounds which contained indoles heterocyclic as the flat aromatic group, benzyloxy substituent at indoles 6 site as the nonhydrophilic group tail, carboxylic derivatives and TZDs bioisosterism substituent at indoles 2 site or 3 site as the hydrophilic group head.

于是根据我们课题组多年来对吲哚生物碱研究的经验,我们设计了以吲哚作为中间平面芳环体系,6位连接苄氧基作为疏水尾部,2位或3位连接羧酸及其衍生物、噻唑烷二酮及其电子等排体的一系列化合物。

Cyclohexylamine is mainly to be made sodium cyclamate, CBS accelerating agent, cyclohexanol, cyclohexanone, caprolactam, acetate fiber and nylon.

环己胺主要用于合成食品甜味剂环己基氨基磺酸钠和橡胶促进剂N-环己基-2-苯并噻唑次磺酰胺。

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