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fentanyl derivatives
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  芬太尼衍生物
     Synthesis and Anesthetic Activity of 3-Methyl Fentanyl Derivatives
     3-甲基芬太尼衍生物的合成及其麻醉活性
短句来源
     ANESTHETIC ACTIVITY OF SOME 4-SUBSTITUTED FENTANYL DERIVATIVES IN MICE
     一些4位取代芬太尼衍生物对小鼠的麻醉活性
短句来源
     Studies on Structure-Activity Relationship of Fentanyl Derivatives by EHMO and Pattern Recognition Method
     EHMO和模式识别法研究芬太尼衍生物的构效关系
短句来源
     Studies on Structure-activity Relationship of Fentanyl Derivatives by T. Kohonen Self-organization Model
     芬太尼衍生物构效关系的自组织人工神经网络研究
短句来源
     SELF-ORGANIZATION NEURAL TREE APPLIED TO STRUCTURE-ACTIVITY RELATIONSHIP OF FENTANYL DERIVATIVES
     自组织神经树用于芬太尼衍生物构效关系的研究
短句来源
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  芬太尼类化合物
     Synthesis, Analgesic Activity and Structure-Activity Relationship of 4-N-Cyclohexyl Analogs of Some Fentanyl Derivatives
     芬太尼类化合物4-N-环己基类似物的合成与镇痛活性及构效关系研究
短句来源
     The Studies on Molecular Electrostatic Potential of Fentanyl Derivatives
     芬太尼类化合物的分子静电势研究
短句来源
     The orientation of the N-phenylpropanamide with respect to piperidine ring plays an important role in the binding of Fentanyl-type analgeties to the opiate receptor. When the N-phenethyl substituent is the antiperiplauar conformation and the torsion angle (C_(11)-C_(12)-N_(15)-C_(16)) is about 100°,Fentanyl derivatives may interact equally well with the receptor.
     4-取代和顺式3-甲基芬太尼类化合物的晶体结构是一个能量较为合理的体系,在该体系下的构象有可能是生物活性构象,即哌啶环1-位苯乙基为伸展构象,哌啶环4-位扭角τ_4(C_(11)—C_(12)—N_(15)—C_(16))为100°左右时有利于与受体相互作用。
短句来源
     CONFORMATIONAL ANALYSIS OF THE μ-OPIATE RECEPTOR AGONIST FENTANYL DERIVATIVES
     芬太尼类化合物与阿片受体相互作用的构象分析
短句来源
     STUDIES ON CRYSTAL STRUCTURES AND STRUCTUREACTIVITY RELATIONSHIPS OF THE 4-SUBSTITUTED FENTANYL DERIVATIVES
     4-取代芬太尼类化合物的晶体结构和构效关系
短句来源
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  “fentanyl derivatives”译为未确定词的双语例句
     SYNTHESIS AND PHARMACOLOGICAL ACTIVITIES OF THE 1-SUBSTITUTED 4-METHOXYCARBONYL FENTANYL DERIVATIVES
     4-甲氧羰基芬太尼1-位衍生物的合成及生物活性
短句来源
     Structure-Activity Relation Study of Fentanyl Derivatives and Multicompontens Quantitative Analysis Using BP and PLS Algorithm
     神经元网络技术和偏最小二乘法在定量分析和构效关系方面的比较
短句来源
     Preliminary pharmacological results showed that analgesic activities of compounds in this series were strong and corresponding to those of 3-methyl fentanyl derivatives and 4-methoxycarbonyl fentanyl derivatives. Compound N-[-1-(2-hydroxy-2-phenylethyl)-3-methl-4-methoxycarbonyl-4-piperidinyl]-N-propionylaniline (18a) was found to be the most potent. Its analgesic activity was 2939 times more potent than that of morphine.
     实验结果表明,该类化合物具有与3-甲基芬太尼类和4-甲氧羰基芬太尼类相当的强效镇痛活性(活性最强的化合物18a镇痛强度为吗啡的2939倍),构效关系更类似于前者。
短句来源
     Using the back-propagation alogrithm and Partial Least-Squares Method the Structure-Activity Relation of Fentanyl derivatives and quantitative analysis of five organic compounds mixtures were studied on the UV Spectrophotometer-PC/AT On-Line system.
     在光度计/计算机联机系统上利用人工种经网络反向传递算法和偏最小二乘法对五组分有机物混合体系的紫外光谱数据和芬太尼构效关系数据同时进行了定性定量分析、对比和研究。
短句来源
     Using the back-propagation alogrithm and Partial Least-Squares Method the Structure-Activity Relation of Fentanyl derivatives and quantitative analysis of five organic compounds mixtures were studied on the UV Spectrophotometer-PC/AT On-Line system.
     在光度计/计算机联机系统上利用人工神经网络反向传递算法和偏最小二乘法对五组分有机物混合体系的紫外光谱数据和芬太尼构效关系数据同时进行了定性定量分析,对比和研究。
短句来源
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  fentanyl derivatives
To the extent that rate-decreasing effects are predictive of antinociceptive effects, these data suggest that some fentanyl derivatives might be useful therapeutics under conditions where tolerance develops to morphine-like opioids.
      
Naltrexone (0.1-1.0?mg/kg) attenuated the effects of OHM3463 and not mirfentanil or OHM3295, suggesting non-opioid mediation of the rate-decreasing effects for the latter two fentanyl derivatives.
      
In untreated pigeons, fentanyl, morphine, naltrexone, ketamine and three fentanyl derivatives (mirfentanil, OHM3463 and OHM3295) decreased rates of key pecking in a dose-related manner.
      
The rate-decreasing effects of fentanyl derivatives in pigeons before, during and after chronic morphine treatment
      
Improving sedation and discomfort with the use of medications such as fentanyl derivatives and propofol may also help improve colonoscopy compliance.
      
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In the present paper, we report the preparation of a series of Fentanyl derivatives which are N-[1-(β-arylalkyl)-4-piperidyl]-N-propionyl aniline, N-[1-(β-phenylet-hyl)-4-piperidyl]-N-amidoaniline, N-[1(-β-phenylethyl)-4-piperidyl]-E-propionylary-lamine, N-[1-(β-arylethyl)-4-tropyl]-N-propionyl aniline and N-1-(β-arylethyl)-4-pyrrolidinyl]-N-propionyl aniline. A total of 22 compounds were synthesized.Pharmacological results showed that most of the compounds in these series possessed morphine-like effects...

In the present paper, we report the preparation of a series of Fentanyl derivatives which are N-[1-(β-arylalkyl)-4-piperidyl]-N-propionyl aniline, N-[1-(β-phenylet-hyl)-4-piperidyl]-N-amidoaniline, N-[1(-β-phenylethyl)-4-piperidyl]-E-propionylary-lamine, N-[1-(β-arylethyl)-4-tropyl]-N-propionyl aniline and N-1-(β-arylethyl)-4-pyrrolidinyl]-N-propionyl aniline. A total of 22 compounds were synthesized.Pharmacological results showed that most of the compounds in these series possessed morphine-like effects in laboratory animals with potencies levels 2~150 times those of morphine.

本文报道了芬太尼类衍生物的化学结构与镇痛活性之间的关系。分别改变了芬太尼中的哌啶环1位氮原子的取代基,N-酰芳胺基及哌啶环等部分结构。药理试验结果表明,大部分化合物均具有吗啡样镇痛活性,其镇痛强度分别为吗啡的2~150倍左右。

The semiempirical self-consistent field MO(INDO)calculations have been undertakenfor 11 4-substituted-fentanyl derivatives.Electronic structure and structure-activityrelationships of these compounds were investigated.Study of the results showed thatmain active site and trend of electronic structure of these compounds are about the sameas that of another type of fentanyl compounds.Some important quantum chemical indicessuch as electron density on piperidyl nitrogen and amide oxygen correlates with...

The semiempirical self-consistent field MO(INDO)calculations have been undertakenfor 11 4-substituted-fentanyl derivatives.Electronic structure and structure-activityrelationships of these compounds were investigated.Study of the results showed thatmain active site and trend of electronic structure of these compounds are about the sameas that of another type of fentanyl compounds.Some important quantum chemical indicessuch as electron density on piperidyl nitrogen and amide oxygen correlates with biologicalactivity.Electric,steric and hydrophobic factors of 4-substituents of these compoundscorrelates with biological activity too.Polar group of 4-substituent not only can interactwith polar site of receptor by charge transfer and/or hydrogen bond formation but alsocan increase negative charge on amide oxygen.

本文对十一个4-取代 Fentanyl 类化合物进行了量子化学(INDO)计算,研究了它们的电子结构及构效关系.结果表明,这些化合物同其他 Fentanyl 类化合物在主要活性部位和电子结构趋势上基本相同.酰胺氧原子是最重要的负电中心,哌啶氮原子在季铵化后发挥正电中心作用.4-取代基的极性基团可能以电荷转移作用或氢键接受体形式与受体极性部位结合,并能影响其他活性部位电子密度,另外,4-取代基的立体因素与疏水因素同生物活性相关.

X-ray crystallography and computer-assisted conformational analysis and computer graphics studies were performed for seven Fentanyl-type potent agonist of opiate receptor. The results obtained demonstrate that there is a good agreement between the experimentally determined (by X-ray) and the calculated (by DPCILO) conformation of Fentanyl derivatives. The orientation of the N-phenylpropanamide with respect to piperidine ring plays an important role in the binding of Fentanyl-type analgeties...

X-ray crystallography and computer-assisted conformational analysis and computer graphics studies were performed for seven Fentanyl-type potent agonist of opiate receptor. The results obtained demonstrate that there is a good agreement between the experimentally determined (by X-ray) and the calculated (by DPCILO) conformation of Fentanyl derivatives. The orientation of the N-phenylpropanamide with respect to piperidine ring plays an important role in the binding of Fentanyl-type analgeties to the opiate receptor.When the N-phenethyl substituent is the antiperiplauar conformation and the torsion angle (C_(11)-C_(12)-N_(15)-C_(16)) is about 100°,Fentanyl derivatives may interact equally well with the receptor. On the basis of conformational analysis and molecular graphics fit the model for the requirements of the receptor has also been discussed.

本文用X光衍射结晶学,计算机辅助构象分析和分子图形学方法,对芬太尼类μ型阿片受体激动剂中七个典型代表物进行了研究。结果表明,芬太尼类化合物哌啶环4位丙酰苯胺基位置与生物活性有关。4-取代和顺式3-甲基芬太尼类化合物的晶体结构是一个能量较为合理的体系,在该体系下的构象有可能是生物活性构象,即哌啶环1-位苯乙基为伸展构象,哌啶环4-位扭角τ_4(C_(11)—C_(12)—N_(15)—C_(16))为100°左右时有利于与受体相互作用。并在构象分析和分子图形拟合的基础上,提出了芬太尼类化合物与阿片受体之间相互作用的结构要求。

 
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