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非甾体抗炎药。第16部分:立体异构的3-芳基-联苯基-羟基丙酸

Nonsteroidal antiinflammatory agents. Part 16: Stereomeric 3-aryl-biphenylyl-hydroxy-propionic acids.

作者信息

Guarnieri A, Burnelli S, Varoli L, Ghedini N, Scapini G, Ferri S, Cavicchini E

出版信息

Pharmazie. 1985 Aug;40(8):529-31.

PMID:4080796
Abstract

As part of a wider research project on structure-activity relationships of chiral arylalkanoic acids, stereomeric aryl- biphenylyl-hydroxypropionic acids 3a-d have been prepared and their antiinflammatory activity evaluated. Diastereomeric racemic erythro- and threo-acids have been synthesized by reaction of alpha-lithiated biphenylyl-acetic acid salts with the appropriate aldehyde. They were separated, and after attribution of their relative configuration by 1H-NMR analysis, resolved. The antiinflammatory activities of the enantiomeric potassium salts were determined by the carrageenan test.

摘要

作为关于手性芳基链烷酸构效关系的更广泛研究项目的一部分,已制备了立体异构的芳基 - 联苯基 - 羟基丙酸3a - d,并评估了它们的抗炎活性。非对映体外消旋赤藓酸和苏阿糖酸通过α - 锂化联苯基乙酸盐与适当的醛反应合成。它们被分离,通过1H - NMR分析确定其相对构型后进行拆分。对映体钾盐的抗炎活性通过角叉菜胶试验测定。

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