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fentanyl derivative
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  “fentanyl derivative”译为未确定词的双语例句
     Fentanyl was extracted at basic pH with cyclohexane-isobutyl alcohol (197:3) with Ro21-2212 added as internal standard and fentanyl derivative as earner. The drug was back-extracted in H2SO4, then the extract was made basic and recxtracted with ethyl ether-dichloromethane (9:1).
     以Ro21-2212作内标,芬太尼的同系物作载体,在碱性条件下用环己烷-异戊醇(197:3)提取,药物反提至硫酸溶液中,碱化后再用乙醚-二氯甲烷(9:1)提取。
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  相似匹配句对
     TRANSDERMAL FENTANYL
     芬太尼缓释透皮贴剂
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     The Note of Derivative
     关于导数的注解
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     Fullerene and its derivative
     富勒烯及其衍生物
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     Effects of fentanyl on haemorheology
     芬太尼对血液流变学的影响
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  fentanyl derivative
Mirfentanil is a fentanyl derivative with non-opioid actions, including non-opioid antinociceptive effects in rhesus monkeys.
      
Pharmacological profile of a potent, efficacious fentanyl derivative in rhesus monkeys
      
The first of these appeared in California in the late 1970s, a fentanyl derivative called China White that is still around today.
      


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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