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杂环化合物的研究。XXV. 稠合咪唑体系的苯基衍生物:抗炎活性。

Research on heterocyclic compounds. XXV. Phenyl derivatives of fused imidazole systems: antiinflammatory activity.

作者信息

Abignente E, De Caprariis P, Luraschi E, Marmo E, Berrino L, Lo Sasso C

机构信息

Dipartimento di Chimica Farmaceutica e Tossicologica, Facoltà di Farmacia, Università di Napoli, Italia.

出版信息

Res Commun Chem Pathol Pharmacol. 1989 Jul;65(1):35-56.

PMID:2789419
Abstract

A group of seven acidic phenyl derivatives of some fused imidazole systems were subjected to a series of tests in vivo in order to evaluate their pharmacological activity. Antiinflammatory activity was studied by means of the carrageenin-induced rat paw edema. Hot plate test and writhing induced by acetic acid in mice were used to evaluate analgesic activity. Yeast-induced hyperthermia in rats was employed to study antipyretic action. Irritative and ulcerogenic action on the rat gastric mucosa was examined at higher doses. The antiaggregating activity and the inhibition of platelet malondialdehyde production were studied in vitro. All experimental results are discussed from the point of view of structure-activity relationships and mode of action.

摘要

为了评估其药理活性,对一些稠合咪唑系统的七种酸性苯基衍生物进行了一系列体内试验。通过角叉菜胶诱导的大鼠足爪水肿研究抗炎活性。利用热板试验和小鼠醋酸诱导的扭体反应来评估镇痛活性。采用酵母诱导的大鼠体温过高来研究解热作用。在较高剂量下检测对大鼠胃黏膜的刺激和致溃疡作用。在体外研究抗聚集活性和对血小板丙二醛生成的抑制作用。从构效关系和作用方式的角度讨论了所有实验结果。

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