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新型噻唑烷酮类化合物作为强效抗炎和镇痛药。

Novel thiazolidinones as potent anti-inflammatory and analgesic agents.

作者信息

Tandon M, Kumar P, Pande K, Bhalla T N, Barthwal J P

出版信息

Pharmacology. 1985;31(5):260-7. doi: 10.1159/000138130.

DOI:10.1159/000138130
PMID:3877940
Abstract

Various new butyridenyl-2-hydroxybenzylidenyl-1,3-thiazolidinones were synthesized and characterized by elemental analyses, IR and PMR spectral data. The compounds were evaluated for their ability to afford protection against inflammation by carrageenin-induced oedema and cotton pellet implantation in albino rats of either sex. The active derivatives of the present series were also tested for their analgesic activity against aconitine-induced writhing in albino mice and ulcerogenic activity in albino rats. The toxicity of the compounds was reflected by determination of their approximate LD50 in albino mice. An attempt has also been made to correlate their structure-activity relationship.

摘要

合成了各种新型的丁烯基-2-羟基亚苄基-1,3-噻唑烷酮,并通过元素分析、红外光谱和核磁共振光谱数据对其进行了表征。通过角叉菜胶诱导的水肿和棉球植入法,对这些化合物在雌雄白化大鼠中提供抗炎保护的能力进行了评估。还测试了本系列活性衍生物对白化小鼠乌头碱诱导的扭体反应的镇痛活性以及对白化大鼠的致溃疡活性。通过测定化合物在白化小鼠中的近似半数致死量来反映其毒性。还尝试了关联它们的构效关系。

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