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5-(4-[芳基(芳基偶氮)亚甲基氨基]苯基)-1,3,4-恶二唑-2(3H)-硫酮的抗炎和镇痛活性

Anti-inflammatory and analgesic activities of 5-(4-[aryl(aryl azo)methyleneamino]phenyl)-1,3,4-oxadiazole-2(3H)-thiones.

作者信息

Kalsi R, Bhalla T N, Parmar S S, Barthwal J P

机构信息

Jawaharlal Nehru Laboratory of Molecular Biology, Department of Pharmacology, King George's Medical College, Lucknow, India.

出版信息

Pharmacology. 1989;39(2):103-8. doi: 10.1159/000138584.

DOI:10.1159/000138584
PMID:2798549
Abstract

Various new formazans of substituted oxadiazole 2(3H)-thiones were tested for their anti-inflammatory activity against carrageenin-induced paw oedema in albino rats. Among these, two most potent derivatives were evaluated in detail using cotton pellet implantation methods in albino rats of either sex. These two active analogues were also tested for their analgesic activity in albino mice and ulcerogenic liability in albino rats. The toxicity of the compounds was assessed by determination of their approximate LD50 value in albino mice. An attempt has also been made to establish the structure-activity relationship.

摘要

对各种取代恶二唑2(3H)-硫酮的新型甲臜进行了测试,以研究其对卡拉胶诱导的白化大鼠爪肿胀的抗炎活性。其中,使用棉球植入法在雌雄白化大鼠中对两种最有效的衍生物进行了详细评估。还对白化小鼠测试了这两种活性类似物的镇痛活性,并对白化大鼠测试了其致溃疡倾向。通过测定化合物在白化小鼠中的近似半数致死量值来评估其毒性。还尝试建立构效关系。

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