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methyl fentanyl
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  相似匹配句对
     Synthesis of 3-methyl [carbonyl-~(14)C] fentanyl
     3-甲[羧基-~(14)C]芬太尼的合成
短句来源
     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
     TRANSDERMAL FENTANYL
     芬太尼缓释透皮贴剂
短句来源
     Chemistry of Methyl-cyclotpentadienes
     甲基环戊二烯的化学
短句来源
     Synthesis of Methyl Orthoformate
     原甲酸三甲酯制备方法的改进
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Since introduction of a methyl group in the 3-position of piperidine ring of 4-phenylpiperidine analgesics and replacement of phenylethyl group in the 1-position of piperidine ring of fentanyl by some substituents can enhance analgesic activity, we already synthesized some 3-methyl derivatives of fentanyl e. g., N-[1-(2-phenylethyl)-3-methyl-4-piperidyl]-N-phenylpropanamide(7209, simply named as 3-methyl fentanyl) and others (7207, 7222, 7210). In view of their higher analgesic activity than that of fentanyl,...

Since introduction of a methyl group in the 3-position of piperidine ring of 4-phenylpiperidine analgesics and replacement of phenylethyl group in the 1-position of piperidine ring of fentanyl by some substituents can enhance analgesic activity, we already synthesized some 3-methyl derivatives of fentanyl e. g., N-[1-(2-phenylethyl)-3-methyl-4-piperidyl]-N-phenylpropanamide(7209, simply named as 3-methyl fentanyl) and others (7207, 7222, 7210). In view of their higher analgesic activity than that of fentanyl, studies on derivatives of 3-methyl fentanyl were further performed. Pharmacological results showed that some compounds in this series have extremely potent analgesic activity with typical morphine-like action. The structure-activity relationships of these compounds are discussed, compound N-[1-(2-hydroxy-2-phenylethyl]-3-methyl-4-piperidyl]-N-phenylpropanamide (7302) was found to be the most potent analgesic agent in this series. Its analgesic ED_(50) value was 0.0022mg/kg and the analgesic activity was 28 times more potent than that of fentanyl and 6318 times than morphine.

本文报道了N-[1-(β-苯乙基)-3-甲基-4-哌啶基]-N-丙酰苯胺(7209)和N-[1-(β-羟基-β-苯乙基)-3-甲基-4-哌啶基]-N-丙酰苯胺(7302)等一系列3-甲基芬太尼类衍生物的合成及镇痛活性。绝大部分该类衍生物均具有典型的吗啡样镇痛活性,是一类结构较简单、易于合成、镇痛作用极强的麻醉镇痛剂。化合物7302的ED_(50)为0.0022mg/kg(ip,小鼠,热板法),比芬太尼强28倍,竟达吗啡的6318倍,为我们至今合成该类衍生物中作用最强者。

The synthesis of some 4-N-propionyl analogs of cis-3-methylfentanyl by acyl chloride method, anhydride method, mixed anhydride method and DCCmethod is reported. The ethyl group in 4-N-propionyl portion of cis-3-methylfentanyl was substituted by some groups with different electronic property. In mouse hotplate test. all compounds showed typical morphine-like action with analgesic potency cor-responding to 49~1963 times that of morphine. Compound 3 was found to exhibit higheranalgesic activity than cis-3-methyl...

The synthesis of some 4-N-propionyl analogs of cis-3-methylfentanyl by acyl chloride method, anhydride method, mixed anhydride method and DCCmethod is reported. The ethyl group in 4-N-propionyl portion of cis-3-methylfentanyl was substituted by some groups with different electronic property. In mouse hotplate test. all compounds showed typical morphine-like action with analgesic potency cor-responding to 49~1963 times that of morphine. Compound 3 was found to exhibit higheranalgesic activity than cis-3-methyl fentanyl. Semiempirical INDO calculationshave been undertaken for 4 typical compounds and it was found that as a result of in-troduction of chlorovinyl, compound 3 exhibited characteristics of electronic structuredifferent from that of cis-3-methyl fentanyl. The relationships between analgesic activityand the electronic structure of these compounds were discussed.

以不同电性的基团取代顺-3-甲基芬太尼中4-N-丙酰基上的乙基,合成某些顺-3-甲基芬太尼的结构类似物。药理试验结果表明,所合成的化合物均有典型的吗啡样作用。化合物3的镇痛活性略强于顺-3-甲基芬太尼。应用半经验的INDO方法对4个代表化合物进行了量子化学计算,讨论了电子结构与镇痛活性间的关系,化合物3由于氯乙烯基的引入具有与顺-3-甲基芬太尼不同的电子结构特征,氯乙烯基可能作为电子接受体参与了与受体的作用。

The synthesis, separation of diastereo-isomers and analgesic activities of some analogs of N-[1-(2-phenylethyl)-3-methyl-4-methoxycarbonyl-4-piperidinyl]-N-propionylaniline (3-methyl-4-methoxycarbonyl fentanyl) were reported. 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...

The synthesis, separation of diastereo-isomers and analgesic activities of some analogs of N-[1-(2-phenylethyl)-3-methyl-4-methoxycarbonyl-4-piperidinyl]-N-propionylaniline (3-methyl-4-methoxycarbonyl fentanyl) were reported. 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. The structure-activity relationship in this series is similar to that of 3-methyl fentanyl series. Usually, the cis-isomer has higher activity than trans-isomer but in individual cases, activity of the trans-isomer is higher than the cis-isomer. However, the analgesic potency ratio between diastereoisomer in this series is smaller than in 3-methyl fentanyl series. It seems that the introduction of 4-methoxycarbonyl group into molecules of 3-methyl fentanyl derivatives may reduce selectivity of action of 3-methyl fentanyl.

报道某些3-甲基-4-甲氧羰基芬太尼类似物的合成,顺反异构体的分离及其镇痛活性。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。顺式异构体的活性通常强于反式,且二者强度比较小,提示4-甲基羰基引入到3-甲基芬太尼类化合物分子中降低了3位甲基对阿片受体作用的选择性。

 
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