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菲并烷酸,IV:丙酸的2-、3-和9-菲基以及9-氯-3-菲基衍生物的合成与抗炎活性

Phenanthrylalkanoic acids, IV: Syntheses and antiinflammatory activity of 2-, 3-, and 9-phenanthryl- and 9-chloro-3-phenanthryl derivatives of propanoic acid.

作者信息

Fernández F, González C, Gómez G, López C, Medina L, Calleja J M, Cano E

机构信息

Departmento de Química Organica, Facultad de Farmacia, Universidad de Santiago, Spain.

出版信息

Arch Pharm (Weinheim). 1990 Apr;323(4):239-42. doi: 10.1002/ardp.19903230412.

Abstract

The phenanthrylethanols 2a-d were obtained by reduction of the acetyl derivatives 1a-d and converted, through the phenanthrylethyl halides 3a-d and 4b, into the nitriles 5a-d, whose acid hydrolysis afforded the acids of the title, 6a-d. The antiinflammatory activity of these acids was measured on the carrageenin-induced edema and found as 1/3 (6a), 1/43 (6b), 1/5 (6c), and 1/7 (6d) of that of fenbufen.

摘要

通过还原乙酰衍生物1a - d得到菲基乙醇2a - d,并通过菲基乙基卤化物3a - d和4b将其转化为腈5a - d,腈5a - d经酸性水解得到标题中的酸6a - d。在角叉菜胶诱导的水肿实验中测定了这些酸的抗炎活性,发现其活性分别为芬布芬的1/3(6a)、1/43(6b)、1/5(6c)和1/7(6d)。

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