唑

In this thesis, 1, 5-diaryl-3-pyrazilidinones, 1, 5-diaryl-3-hydroxypyrazoles and 3-(2, 3, 4, 6-tetraacetyl-β-D-glucopyranos-1-yl)-1, 5-diaryl-1H-pyrazoles are designed and synthesized.1, 5-diaryl-3-pyrzolidinones were obtained by condensation of 3-arylpropenates and phenylhydrazine or fluorophenylhydrazine under the catalysis of sodium methylate and the yields were about 55-80%.

在本文中，设计合成了1，5-二芳基-3-吡唑烷酮化合物、1，5-二芳基-3-吡唑烷酮化合物和3-(2，3，4，6-四乙酰基-β-D-吡喃葡萄糖-1-基)-1，5-二芳基吡唑化合物。以3-芳基-2-丙烯酸酯为原料，与芳基肼在醇钠的催化作用下，反应可以生成1，5-二芳基-3-吡唑烷酮，产率在55%以上。

Objective: To explore the effect of intramuscular injection of midazolam before intravertebral anesthesia on sedation luring operation and amnesia after operation. Methods: Selected 180 ASA cases at 1~2 stage with lower extremity surgery under combined spinal and epidural anaesthesia, and randomly divided them into midazolam group and phenobarbital sodium group. Gave patients in midazolam group intramuscular injection of midazolam at 0.1mg/kg 10 min earlier before operation, while gave patients in phenobarbital sodium group 0.1 g phenobarbital sodium 30 mm earlier.

目的：探讨椎管内麻醉前肌注咪唑安定对术中的镇静作用和对术后遗忘的影响：方法：选择ASA1~2级择期在腰硬联合阻滞下行下肢手术的患者180例，随机分为咪唑安定组和苯巴比妥钠组，咪唑安定组患者入室后（实施麻醉前10min）肌内注射咪唑安定0.1mg/kg，苯巴比妥钠组患者入室前30min肌内注射苯巴比妥钠0.1g。

The ammonia was evaporated under decreasing pressure, and the precipitate was filtered off and the liquid was poured into hot saturated picric acid solution to get picrate with a yield of 85.0%. The optimum process starting from imidazole-4,5-dicarboxylic acid was: imidazole-4,5-dicarboxylic acid in acetic anhydride was refluxed to get imidazole-4-carboxylic acid, and the product was esterification in ethanol with a catalyzer of concentrated sulfuric acid to get ethyl imidazole-4-carboxylate, at last the compound above was reduced by LiAlH4 in ether at room temperature to get the target compound, the total yield of this route was 49.6%.

以4，5-二羧酸咪唑为原料的较佳工艺：1 脱羧反应：4，5-二羧酸咪唑40g，醋酐1200ml，回流10h，过滤并将滤液浓缩至干，所得固体加至50%的乙醇溶液回流，过滤并将滤液自然冷却过夜，过滤得固体；2 酯化反应：4(5)-羧酸咪唑50g，乙醇1000ml和浓硫酸60ml，加热回流2h，5%浓度NaOH溶液调节至pH＝8，减压浓缩至干，加入少量水回流，自然冷却过夜并过滤得固体；3 还原反应：LiAlH410g，乙醚300ml和4(5)-羧酸咪唑乙酯28g，常温反应1.5h，小心滴加25ml水后过滤，滤渣溶于300ml甲醇中并过滤，收集所得乙醚和甲醇滤液浓缩至干，将所得固体溶于300ml乙醇中加热回流，后将溶液浓缩至约30ml，冷却并过滤得固体，该路线总收率为49.6%。

In the first one , Our experiment team use ethanol liquor as solvent and achieve the process of racemization of dextrorotatory imidazole in sodium hydroxide environment.

四咪唑的原料成本要比左旋咪唑低50%，其临床驱虫效果也要比左旋咪唑小50%。左旋咪唑的疗效是消旋体的两倍，毒性低一半。

Toxic effects of twelve pesticides（abamectin, endosulfan, diflubenzuron, danitol, tricyclazole, fluroxypyr, imazalil, tebuconazole, sulfapyridine, sulfamethoxazole, sulfamethazine and sulfadiazine）at low concentration（0.01mg·L-1） on the development of sea urchinembryos were investigated in this work, and the correlation between n-octanol/water partition coefficientand relative lethality rate was investigated.

为了研究低浓度下农药对海胆胚胎的毒性影响，以及正辛醇/水分配系数与致死率的关系，实验研究了12种常见农药（阿维菌素、硫丹、除虫脲、甲氰菊酯、三环唑、使它隆、抑霉唑、戊唑醇、磺胺吡啶、磺胺甲噁唑、磺胺二甲嘧啶和磺胺嘧啶）在低浓度（0.01mg.L-1）下对光棘球海胆胚胎发育的急性毒性影响。

It has been shown that tautomerism has a significant effect on the QSAR modelling, and the models obtained from 1H-indazol tautomeric form always represent higher quality than those from 2H-indazol tautomer, which indicates that 1H-indazol tautomer of the indazolyl urea is probably the active form when binding with the TRPV1 channel protein. It has also been demonstrated that the theoretical descriptors derived from electrostatic potentials on molecular surface together with the GETAWAY descriptors can be well used to express the quantitative structure-activity relationship of indazolyl urea TRPV1 channel antagonists.

结果表明：互变异构对QSAR结果具有一定的影响，采用1H-吲唑异构形式得到的模型，在质量上均高于采用2H-吲唑异构体，预示着1H-吲唑异构体更有可能是吲唑脲类分子的活性异构形式；分子表面静电势参数结合GETAWAY参数可以较好地用于描述TRPV1通道拮抗剂分子结构与其活性间的定量关系。

Reactions of 5-amino-lH-pyrazoles with aromatic and aliphaticα-bromoacetophenones, followed by acid-mediated iminative cyclization and the ensuing tautomerization, produced methylthio-imidazolo[1,2-b]pyrazoles 6a-6g.

咪唑并[1，2-b]吡唑甲硫醚类化合物经过室温下H_2O_2/CH_3COOH温和氧化，得到咪唑并[1，2-b]吡唑甲基亚砜类化合物7a-7g。

The chapter 6 makes a study on the design and synthesis of new glycosides, which prepared from imidazole, thiazole and tetrazole aglycones mentioned above and glucose derivatives by phase transfer catalysis under the moderate reaction condition.

我们以合成的新杂环化合物作为糖的配基，用相转移催化法合成了25个糖苷类化合物。其中包括4个咪唑氮糖苷，12个含有噻唑环的糖苷，6个含有噻唑环的糖酯，3个四氮唑糖苷。

Methods Seven probe drugs were incubated with or without methyl protodioscin respectively in human microsomes. The specific substrates used in this study were caffeine (CYP1A2), dextromethorphan (CYP2D6), tolbutamide (CYP2C9),-mephenytoin (CYP2C19), chlorzoxazone (CYP2E1), coumarin (CYP2A6) and midazolam (CYP3A4). The concentrations of the substrate metabolites (paraxanthine, dextrorphan, 4-hydroxytolbutamide, 4-hydroxymephenytoin, 6-hydroxychlor-zoxazone, 7-hydroxycoumarin and 1-hydroxymidazolam) were determined by HPLC and LC-MS/MS. Results MPD 1-10 μmolL^(-1 had no significant inhibition on the activities of the seven cytochrome P450 enzymes.

将MPD和CYP450酶7种亚型的特异性探针底物咖啡因(CYP1A2)、右美沙芬(CYP2D6)、甲苯磺丁脲(CYP2C9)、s-美芬妥因(CYP2C19)、氯唑沙宗(CYP2E1)、香豆素(CYP2A6)及咪达唑仑(CYP3A4)与人肝微粒体进行孵化反应，采用HPLC和LC-MS/MS法测定对应的7种代谢产物（1，7-二甲基黄嘌呤、去甲右美沙芬、4-羟基甲苯磺丁脲、4-羟基美芬妥因、6-羟基氯唑沙宗、7-羟基香豆素和1-羟基咪达唑仑）的浓度，通过与对照组比较，确定MPD对以上7种酶活性的影响。

The benezothiazolocoumarin dyes substituted with chlorine on 5'-position also showed bathochromic shift of the maximum absorption and fluorescence emission.

这9只染料用於涤纶染色有很好的应用性能，差别不大；恶唑环结构和喹唑酮结构的染料耐光牢度明显好於噻唑环结构和咪唑环结构的染料。

However, as the name（read－only memory）implies, CD disks cannot be written onorchanged in any way.

然而，正如其名字所指出的那样，CD盘不能写，也不能用任何方式改变其内容。

Galvanizes steel pallet is mainly export which suits standard packing of European Union, the North America. galvanizes steel pallet is suitable to heavy rack. Pallet surface can design plate type, corrugated and the gap form, satisfies the different requirements.

镀锌钢托盘多用于出口，替代木托盘，免薰蒸，符合欧盟、北美各国对出口货物包装材料的法令要求；喷涂钢托盘适用于重载上货架之用，托盘表面根据需要制作成平板状、波纹状及间隔形式，满足不同的使用要求。