抗炎药。1. 2-氨基-3-苯甲酰基苯乙酸的合成及抗炎活性

Antiinflammatory agents. 1. Synthesis and antiinflammatory activity of 2-amino-3-benzoylphenylacetic acid.

作者信息

Welstead W J, Moran H W, Stauffer H F, Turnbull L B, Sancilio L F

出版信息

J Med Chem. 1979 Sep;22(9):1074-9. doi: 10.1021/jm00195a012.

Abstract

The synthesis and antiinflammatory activity of 2-amino-3-benzoylphenylacetic acid are described. This compound was postulated to be an active metabolite of 7-benzoylindoline in order to explain the unexpected antiinflammatory activity of the latter compound. Metabolism studies on 14C-labeled 7-benzoylindoline did not confirm this hypothesis. Nevertheless, 2-amino-3-benzoylphenylacetic acid, its ethyl ester, and the sodium salt show potent antiinflammatory activity in pharmacological models.

摘要

描述了2-氨基-3-苯甲酰基苯乙酸的合成及其抗炎活性。为了解释后一种化合物意外的抗炎活性，推测该化合物是7-苯甲酰基吲哚啉的活性代谢产物。对14C标记的7-苯甲酰基吲哚啉的代谢研究并未证实这一假设。尽管如此，2-氨基-3-苯甲酰基苯乙酸及其乙酯和钠盐在药理模型中显示出强效抗炎活性。