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2-羟基乙酰基-7-乙酰基呫吨酮的合成,一种具有抗过敏性、镇痛和抗炎活性的新型呫吨酮衍生物。

Synthesis of 2-hydroxyacetyl-7-acetyl-xanthone, a new xanthone derivative endowed with antianaphylactic, analgesic, and antiinflammatory activities.

作者信息

Bianco A, Passacantilli P, Righi G, Brufani M, Cellai L, Marchi E, Milani M R

机构信息

Dipartimento di Chimica, Università La Sapienza, Roma.

出版信息

Farmaco. 1989 Jun;44(6):547-54.

PMID:2803446
Abstract

2-Hydroxyacetyl-7-acetylxanthone (V), a new xanthone derivative, was synthesized in four steps starting from xanthene, by two synthetic approaches. The new compound displayed antianaphylactic activity in the PCA test and in the anaphylaxis shock test in rats. It also displayed analgesic activity in the writhing test in mice, and antiinflammatory activity in the carrageenin edema test in rats. The activity of the new compound has been tentatively interpreted on the basis of its chemical and structural analogy with known drugs.

摘要

2-羟基乙酰基-7-乙酰基呫吨酮(V)是一种新的呫吨酮衍生物,以呫吨为起始原料,通过两种合成方法经四步反应合成得到。该新化合物在大鼠的被动皮肤过敏反应(PCA)试验和过敏性休克试验中表现出抗过敏活性。在小鼠扭体试验中显示出镇痛活性,在大鼠角叉菜胶水肿试验中表现出抗炎活性。基于其与已知药物的化学和结构相似性,对该新化合物的活性进行了初步解释。

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