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咪唑

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But in the + moiety, the three benzimidazole rings shared the whole space equally, the dihedral angel among them is about 120°, just like three fan blades of an airscrew, the molecular structure appear gear-like shape.

X-射线单晶衍射测试、红外、紫外等方法确定了三(2-苯并咪唑亚甲基)胺的Fe和Co配合物的结构,由晶体结构发现金属配位情况不同、配合物在结构上存在着差异,Fe为八面体构型,而Co为三角双锥构型;其次,两配合物中的苯并咪唑环间夹角不同,配合物中包含N2和N4的两个苯并咪唑环间夹角仅为9.41(0.11),几乎构成一个平面,呈蝴蝶形;后者Co三个苯并咪唑环几乎平分了整个空间,它们之间的夹角约为120,呈三扇叶螺旋桨式构型,为齿轮形。

Ophenyl phenol,ophenyl phenol sodium salt tetrahydrate,7ADCA,2ethyl phenyl hydrazine hydrochloride,2,3dihydrofuran,7ethyl3(2hydroxy ethyl)indole,methyl ester of etodolac; 1,8diethyl1,3,4,9tetrahydropyrano[3.4b] indole1acetic acid methyl ester,5chloro2methoxy benzoic acid,4(2aminoethyl)benzene sulfonamide,5cyano phthalide,phthalhydrazide,9thioxanthenone,n[(1,4benzodioxane2yl)carboxyl]piperazine HCL,2chloro4amino6,7dimethoxyquinazoline,2chloro benzimidazole,1(4fluorobenzyl)2chlorobenzimidazole,2methylthio4pyrimidone,5amino4imidazole carboxamide HCL,6chloro2hexanone,11oxo6.11hydrodibenzothiepin,6,11dihydrodibenzooxepin11one,10,11dihydrodibenzocyclohepten5one;dibenzosuberone,dibenzo cyclohepten5one;dibenzosuberenone,3,5dihydroxy benzoic acid,3,5dihydroxy benzyl alcohol,2mercapto benzimidazole,3,4dihydroxy benzaldehyde,3,4dihydroxy benzonitrile,2amino5chloro benzonitrile,2(4chlorophenoxy)ethyl chloride,2(4chloro phenoxy)tert,butane,ditrimethylol propane;DTMP,2,2bis(4hydroxyphenyl)butane; bisphenol B,1,1'bis(4hydroxyphenyl)cyclohexane;bisphenol Z,tetrabromobisphenolS,3,5ditertbutyl salicylic acid,3,4,5trihydroxy benzoic acid stearyl ester,1,2,4trimethoxybenzene.

华业公司产品:邻苯基苯酚,邻苯基苯酚钠盐,7氨基3去乙酰氧基头孢烷酸,邻乙基苯肼盐酸盐,2,3二氢呋喃,7乙基色氨醇,依托度酸甲酯,5氯2甲氧基苯甲酸,4(2氨乙基)苯磺酰胺,5氰基苯酞,双酮酞嗪,9噻吨酮,N〔(1,4苯并二恶烷2基)羰基〕哌嗪盐酸盐,2氯4氨基6,7一二甲氧基喹唑啉,2氯苯并咪唑,1(4氟苄基)2氯苯并咪唑,2甲硫基4嘧啶酮,5氨基咪唑4 甲酰胺盐酸盐,6氯2已酮,11氧6.11二氢苯并〔b.c〕虑平,11氧代6,11二氢二苯并氧杂卓,10,11二氢二苯并环庚烯5酮,二苯并环庚烯5酮,3,5二羟基苯甲酸,3,5二羟基苯甲醇,2巯基苯并咪唑,3,4二羟基苯甲醛,3,4二羟基苯腈,2氨基5氯苯腈,2(4氯苯氧基)1氯乙烷,2(4氯苯氧基)叔丁烷,双丙烷,2,2二(4羟基苯基)丁烷;双酚B,1,1'双(4羟基苯基)环己烷;双酚Z,2[3,5二溴4(2,3二溴丙氧基)]苯砜,3,5二叔丁基水杨酸,3,4,5三羟基苯甲酸十八烷基脂,1,2,4三甲基氧基苯。

The initial SAR studies indicated:(1) the presence of a linker of methene at the N-1 may be beneficial to anti-HIV activity, while longer chain could enhance toxicity;(2) substituted phenyl at the C-2 could reduce toxicity;(3) 6-substituted benzimidazoles generally showed higher anti-HIV activity than 5-substuted ones;(4) the presence of a halogenated benzyl ring at the N-l would enhance anti-HIV potency and decrease cytotoxicity.

初步构效分析提示:(1)苯并咪唑环1位侧链间隔基为亚甲基时活性最好,侧链延长,毒性增大;(2)苯并咪唑2位侧链无间隔基毒性相对较低;(3)苯并咪唑6位取代活性高于5位取代;(4)苯并咪唑1位芳环用卤素取代,毒性明显降低。

The initial SAR studies indica ted:(1)the presence of alinker of methene at the N-1may be beneficial to anti-HIV activity,while longer chain could enhance toxicity;(2)substituted phenyl at the C-2could reduce toxicity;(3)6-substituted benzimidazoles generally showed higher anti-HIV activity than 5-substuted ones;(4)the presence of ahalogenated benzyl ring at the N-l would enhance anti-HIV potency and decrease cytotoxicity.

初步构效分析提示:(1)苯并咪唑环1位侧链间隔基为亚甲基时活性最好,侧链延长,毒性增大;(2)苯并咪唑2位侧链无间隔基毒性相对较低;(3)苯并咪唑6位取代活性高于5位取代;(4)苯并咪唑1位芳环用卤素取代,毒性明显降低。

Intravoneous injection of 0.5mg/kgBW jingsongling cause the 60 minutesrelaxation of goat gastric motor.The effects of jingsongling on the gastric motor ofgoat is major of effects of α2 -adrenoceptor agonist,as well as that of α1 -adrenoceptor agonist,the effects of α1 -adrenoceptor agonist concentrate at thecardic and pylorus;the function of α2 -adrenoceptor exit widely at cardic,pylorus,rumen,reticulum,omasum and abomasum,the function at different part is not the same.The lowestdose of jingsonglinginhibiting the amplitude and frequency of the gastricmyoelectric is 0.01mg/kgBW;the influence of jingsonglingto the gastricmotility of goat is dose-dependent,and the amplitude regain after the frequency ofgastric myoelectriv wave.When the goat revived,the gastric motor function is notreach the level of the normal;the major reason ofjingsongling cause the goat gastricrelaxation is the amplitude renew slowly.The intravoneous injection ofjingsonglingfirst,after 5 minutes,intravoneous injection the antagonist,the effect of prazosin and idazoxan mixed is best,which can fast reversal of theinhibition of jingsongling on the gastric motor of goat,the effects of idazoxan isgood,and the prazosin block the effection of jingsongling is better than that ofxylazine,especially at cardia and pylorus.When intravoneous injection of0.5mg/kgBW idazoxan and/or prazosin only,the amplitude of gastric myoelectric ingoat increases at a certain degree,but the frequency is not changed.

静脉注射0.5mk/kgBW的静松灵引起山羊胃蠕动弛缓长达60分钟;静脉注射0.5mg/kgBW的静松灵对山羊胃蠕动机能的影响是以α2肾上腺素受体作用为主的,兼有α1肾上腺素受体的作用,而且静松灵的α1肾上腺素受体的作用主要集中在幽门和贲门;α2肾上腺素受体的作用广泛存在于贲门、瘤胃、网胃、瓣胃、皱胃和幽门中,不同部位间有功能上的差异;静注0.01mg/kgBW的静松灵是对山羊的贲门、瘤胃、网胃、瓣胃、皱胃和幽门的肌电波频率和振幅均产生影响的最低剂量;静注一定剂量的静松灵对山羊胃蠕动的抑制作用与剂量呈相关性;而且山羊胃肌电波振幅的恢复比肌电波频率的恢复慢;苏醒时山羊的胃蠕动机能尚未恢复到正常状态;静松灵引起山羊胃弛缓的主要原因是由于胃肌电波的振幅恢复慢;静注0.5mg/kgBW的静松灵,5分钟后静注0.5mg/kgBW的拮抗剂时,咪唑克生+哌唑嗪的作用最好,能迅速地逆转静松灵对山羊胃蠕动的抑制作用,咪唑克生也有很强的拮抗作用,而哌唑嗪对静松灵的拮抗效果好于对隆朋的拮抗;单独静注0.5mg/kgBW的咪唑克生和/或哌唑嗪时,山羊的瘤胃、网胃、瓣胃、皱胃、贲门和幽门的肌电波振幅有一定程度的增强,而肌电波频率未见变化。

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.

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。

Three kinds of small molecular copper and zinc superoxide dismutase mimics were synthesized with N, N-bis (benzimidazol-2-ylmethyl) amine (N3), N, N-bis (benzimidazol-2-ylmethyl) methylamine(MN3) and N,N-bis (benzimidazol-2-ylmethyl) benzylamine(BN3) as ligands. The com-plexes were characterized by UV, IR and element analysis and the structures were proposed.

模拟铜一锌超氧化物歧化酶的活性中心,以二(2-苯并咪唑)丙烷为桥、二(2-苯并咪唑亚甲基)胺(N3)、二(2-苯并咪唑亚甲基)甲胺(MN3)及二(2-苯并咪唑亚甲基)苄胺(BN3)为配体合成了3种异双核的小分子模型化合物,并进行了紫外、红外表征及元素分析,推测了可能的结构。

Their structures were characterized by IR, 1H NMR, of which 4-chloro- 2-methyl-7-(2-bromoethoxy) isoflavone, 2, 4\'-dimethyl-7-(2-bromo-ethoxy)isoflavone and 2-methyl-7-(2-bromoethoxy) isoflavone are rarely reported so far.4\'-chloro-2-methyl-7-(3-bromopropoxy)isoflavone, 2, 4\'-dimethyl-7-(3-bromo- propoxy) isoflavone, 2-methyl-7-(3-bromopropoxy) isoflavone, 4\'-methoxy-2-methyl-7-(3-bromopropoxy) isoflavone and 4\'-hydroxy-2-methyl-7-(3-bromopropoxy) isoflavone were gained by reacting 7-hydroxy-2-methyl isoflavone derivatives with 1, 3-dibromo- propane, respectively.

第三章(来源:73ABC论文网www.abclunwen.com)在丙酮溶液中以K_2CO_3为碱,使溴乙氧基异黄酮和溴丙氧基异黄酮与咪唑偶合,以较高的产率合成出10种目标化合物:2-甲基-4′-氯-7-2-(1-咪唑基乙氧基异黄酮、2,4′-二甲基-7-2-(1-咪唑基乙氧基异黄酮、2-甲基-7-2-(1-咪唑基乙氧基异黄酮、2-甲基-4′-甲氧基-7-2-(1-咪唑基乙氧基异黄酮、2-甲基-4′-羟基-7-2-(1-咪唑基乙氧基异黄酮、2-甲基-4′-氯-7-3-(1-咪唑基丙氧基异黄酮、2,4′-二甲基-7-3-(1-咪唑基丙氧基异黄酮、2-甲基-7-3-(1-咪唑基丙氧基异黄酮、2-甲基-4′-甲氧基-7-3-(1-咪唑基丙氧基异黄酮、2-甲基-4′-羟基-7-3-(1-咪唑基丙氧基异黄酮,经IR、~1H NMR、~(13)C NMR、元素分析等对其结构进行了表征,10种目标产物均未见文(来源:ABC论文cccccc网www.abclunwen.com)献报道。

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