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芬布芬,一种新型抗炎镇痛药:类似物的合成与构效关系

Fenbufen, a new anti-inflammatory analgesic: synthesis and structure-activity relationships of analogs.

作者信息

Child R G, Osterberg A C, Sloboda A E, Tomcufcik A S

出版信息

J Pharm Sci. 1977 Apr;66(4):466-76. doi: 10.1002/jps.2600660403.

DOI:10.1002/jps.2600660403
PMID:300797
Abstract

One hundred analogs of fenbufen were prepared and tested using the carrageenan, polyarthritis, and UV erythema anti-inflammatory tests and the 2-phenyl-1,4-benzoquinone writhing and inflamed paw pressure analgesic tests. Only three retained the same full spectrum of activity as fenbufen: dl-4-(4-biphenylyl)-4-hydroxybutyric acid, dl-4-(4-biphenylyl)-1,4-butanediol, and 4-biphenylacetic acid. Fenbufen had the same spectrum of activity as aspirin, phenylbutazone, and indomethacin in the five tests. In addition, dose-response derived potencies show fenbufen more potent than aspirin and at least as potent as phenylbutazone in all five tests. Two related compounds were generally similar.

摘要

制备了100种芬布芬类似物,并通过角叉菜胶、多关节炎和紫外线红斑抗炎试验以及2-苯基-1,4-苯醌扭体和炎性爪压力镇痛试验进行测试。只有三种化合物保留了与芬布芬相同的全谱活性:dl-4-(4-联苯基)-4-羟基丁酸、dl-4-(4-联苯基)-1,4-丁二醇和4-联苯乙酸。在这五项试验中,芬布芬与阿司匹林、保泰松和吲哚美辛具有相同的活性谱。此外,剂量反应得出的效价表明,在所有五项试验中,芬布芬比阿司匹林更有效,且至少与保泰松一样有效。两种相关化合物通常相似。

相似文献

1
Fenbufen, a new anti-inflammatory analgesic: synthesis and structure-activity relationships of analogs.芬布芬,一种新型抗炎镇痛药:类似物的合成与构效关系
J Pharm Sci. 1977 Apr;66(4):466-76. doi: 10.1002/jps.2600660403.
2
A new non-steroidal anti-inflammatory analgesic: gamma-oxo (1,1'-biphenyl)-4-butanoic acid (fenbufen). Chemistry and activity of analogs.一种新型非甾体抗炎镇痛药:γ-氧代(1,1'-联苯)-4-丁酸(芬布芬)。类似物的化学结构与活性
Arzneimittelforschung. 1980;30(4A):695-702.
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The pharmacological properties of fenbufen. A review.联苯乙酸的药理特性。综述。
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Pharmacologic properties of fenbufen.芬布芬的药理特性。
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[Anti-inflammatory activity of a non-steroidal anti-inflammatory agent, oxaprozin, in experimental models].
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Arzneimittelforschung. 1980;30(4A):702-7.

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Inflammation. 1976 Dec;1(4):415-38. doi: 10.1007/BF00920340.
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Anhydride prodrug of ibuprofen and acrylic polymers.布洛芬的酸酐前药与丙烯酸聚合物
AAPS PharmSciTech. 2009;10(2):453-8. doi: 10.1208/s12249-009-9228-z. Epub 2009 Apr 21.
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Paediatrics--Part II.儿科学——第二部分。
Postgrad Med J. 1993 Apr;69(810):268-81. doi: 10.1136/pgmj.69.810.268.
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Pharmacokinetics of fenbufen in man.芬布芬在人体中的药代动力学。
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