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酰胺化作用

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Methods: A model to evaluate lymphocyte proliferation stimulated with a polyclonal activator, concanavalin A, was established by vital dye carboxyl fluorescin diacetate succinmidyl ester labeling technique. Effects of the different doses of anisomycin on the lymphocyte proliferation were estimated by flow cytometry and MTT methods. The propidium iodide labeling technique was applied to assay the effect of the different doses of anisomycin on changes of the lymphocyte cell-cycle stimulated by ConA or by phorbol ester plus Ionomycin. The percentage of the expression level of CD69 and CD25 on the activated lymphocytes was evaluated by fluorescin-conjugated monoclonal antibody double labeling technique.

以活体染料羧基荧光素乙酰乙酸琥珀酰亚胺酯染色,建立在多克隆刺激剂刀豆蛋白A刺激下评价小鼠淋巴细胞增殖的模型,通过流式细胞术和MTT法分析茴香霉素在不同剂量下对淋巴细胞增殖的作用;采用碘化丙锭染色分析茴香霉素对ConA或佛波醇酯加离子霉素刺激的小鼠淋巴细胞周期变化的作用;利用荧光标记的单克隆抗体双染技术和流式细胞术观察茴香霉素对小鼠CD3~+T细胞早期及中期活化标志分子CD69和CD25表达的影响。

Tetrachloroterephthalic acid was prepared by chlorinating terephthalic acid, oleumsolvent and iodine catalyst. Tetrachloroterephthalic acid was acylated by sulphurous oxychloride in the presence of DMF to form tetrachloroterephthaloyl chloride. The acyl chloride product was fluorinated by potassium fluoride and esterified by methanol to synthesize dimethyl tetrafluoroterephthalate. The ester was reduced with potassium borohydride and lithium chloride to give tetrafluoroterephthalyl alcohol. The above product was bromated in the hydrobromic acid to obtain 4-bromomethyl-2,3,5,6-tetrafluoro-benzene methanol. 4-Methyl-2,3,5,-6-tetrafluorobenzene ethanol was obtained by reducing the bromide with magnesium. In the exist of DCC and DMAP, tefluthrin was got by the condensation reaction between 4-methyl-2,3,5,6-tetrafluoro-benzene methanol and-(1RS,3RS)- 3-(2- chloro-3,3,3-trifluoro-1-propenyl)-2,2-dimethyl cycolpropanecar-boxylate acid.

对苯二甲酸与氯气在碘存在下以发烟硫酸为溶剂进行氯化制备四氯对苯二甲酸;再以DMF为催化剂与二氯亚砜反应生成四氯对苯二甲酰氯;以氟化钾为氟化剂,环丁砜为溶剂置换氟化,再与甲醇酯化得到四氟对苯二甲酸甲酯;以KBH4-LiCl为还原剂二甲醚为溶剂反应制得四氟对苯二甲基苄醇;以氯苯为溶剂在溴化氢溶液中溴化得到溴化产物;在乙醇溶液中经镁粉还原得到4-甲基-2,3,5,6-四氟苄醇;甲基苄醇与功夫酸在催化剂二环己基碳二亚胺和4-二甲氨基吡啶作用下缩合得到七氟菊酯,总收率达43.6%。

Pharmacological results also indicated that the carbonyl and imino of Z-47 are important to its marked antiinflammatory and analgesic activity. The activity will be reduced or abolished with Z-47 converted to oximes or/and acetamides.

药理结果还表明,Z-47结构中的羰基和仲胺基对Z-47的显著抗炎镇痛作用具有重要的贡献,将Z-47羰基变成肟或/和将Z-47仲胺基酰化都会造成抗炎镇痛作用的降低甚至是丧失。

Methods Activate groups A and C meningococcal polysaccharide with cyanogens bromide and prepare into MenAPS-ADH and MenCPS-ADH derivatives by reacting with 1, 6-adipic acid dihydrazine. Mix MenAPS-ADH and MenCPS-ADH derivatives with purified tetanus toxoid at a certain mass ratio, then add l-ethyl-3(3-dimethylaminopropyl)-carbodiimide to prepare bulks of MenAPS-TT and MenCPS-TT conjugates respectively. Mix the two bulks at a certain ratio, add stabilizer and lyophilize to prepare group A+C meningococcal polysaccharide conjugate vaccine.

A群和C群脑膜炎球菌多糖在溴化氰的活化下,以1,6己二酰肼作为连接子,与精制破伤风类毒素在碳二亚胺作用下结合,再按一定的比例将两者混合,制成A+C群脑膜炎球菌多糖结合疫苗原液,加保护剂冻干后,制成A+C群脑膜炎球菌多糖结合疫苗。

N-methylmaleimide was prepared by using dimethyl sulfate as methylation reagent.The paper investigated the addition of N-methyl-3,4-dibromomaleimide and indolylmagnesium bromide,and then 2-bromo-3-(1H-indolyl-3-yl)-N-methylmaleimide and 3,4-bis(1H-indolyl-3-yl-)-N-methyl-maleimide were obtained.

对吲哚在溴乙烷和镁作用下生成吲哚溴化镁,而后与3,4-二溴-N-甲基马来酰亚胺的加成反应进行了研究,合成了2-溴-3-(1H-吲哚-3)-N-甲基马来酰亚胺,并对反应条件进行了改进,研究了反应温度和原料配比对反应的影响。

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