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某些1-酰基/芳酰基-5-氨基吡唑衍生物的合成、镇痛及抗炎活性

Synthesis, analgesic and anti-inflammatory activities of some 1-acyl/aracyl-5-aminopyrazole derivatives.

作者信息

Gadad A K, Kittur B S, Kapsi S G, Mahajanshetti C S, Rajur S B

机构信息

Department of Medicinal Chemistry, College of Pharmacy, J. N. Medical College, Belgaum, India.

出版信息

Arzneimittelforschung. 1996 Nov;46(11):1082-5.

PMID:8955869
Abstract

A series of 1-acyl/aracyl-3, 4-disubstituted-5-aminopyrazoles (IV) were synthesized by the reaction of 1-acyl/aracylhydrazines (I) with an appropriately substituted ketenedithioacetal (II/III). Compounds IV were tested for their analgesic activity by rat caudal immersion test and anti-inflammatory activity by carrageenin induced edema in rat paw test. 1-Benzoyl-3-mercapto-4-carboxamido-5-aminopyrazole (IVk) proved to be the most active compound of the series in both tests.

摘要

通过1-酰基/芳酰肼(I)与适当取代的烯酮二硫代缩醛(II/III)反应,合成了一系列1-酰基/芳酰基-3,4-二取代-5-氨基吡唑(IV)。通过大鼠尾部浸入试验测试化合物IV的镇痛活性,并通过角叉菜胶诱导的大鼠足爪水肿试验测试其抗炎活性。在这两种试验中,1-苯甲酰基-3-巯基-4-羧酰胺基-5-氨基吡唑(IVk)被证明是该系列中活性最高的化合物。

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