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在寻找新型抗炎药物的过程中:一些含硫醚基团的噻唑并[3,2-a]嘧啶衍生物的合成与抗炎活性

In the search for new antiinflammatory drugs: synthesis and antiinflammatory activity of some Thiazolo(3,2-a)pyrimidine derivatives containing a thioether group.

作者信息

Passarotti C M, Valenti M, Marini M

机构信息

Research Centre, Formenti Group, Origgio, Italy.

出版信息

Boll Chim Farm. 1995 Dec;134(11):639-43.

PMID:8820980
Abstract

Our strategy for the exploration of new NSAIDs starts on the synthesis of derivatives of 5-oxo-5H-Thiazolo [3,2-a] pyrimidines. The compounds were achieved by the following methods: (a) condensation of 2-amino-4-alkylthiomethilthiazole with ethyl 4-chloro-3-oxobutanoate (PPA method), (b) triphenyl phosphonium salts preparation, (c) Wittig-reaction of the salts with suitable aldehyde. Synthesized compounds were screened for antiinflammatory activity in the carrageenin rat paw oedema assay according to Winter et al. Some of the new synthesize compounds, at the dose used (50 mg/Kg) reduced meaningfully the oedema. The pharmacological effect varies according to the administration time.

摘要

我们探索新型非甾体抗炎药(NSAIDs)的策略始于5-氧代-5H-噻唑并[3,2-a]嘧啶衍生物的合成。这些化合物通过以下方法制备:(a)2-氨基-4-烷基硫甲基噻唑与4-氯-3-氧代丁酸乙酯缩合(PPA法),(b)制备三苯基鏻盐,(c)盐与合适的醛进行维蒂希反应。根据温特等人的方法,在角叉菜胶致大鼠足爪水肿试验中对合成的化合物进行抗炎活性筛选。一些新合成的化合物在所用剂量(50mg/kg)下能显著减轻水肿。药理作用随给药时间而变化。

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