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3,3'-二[1,3-噻唑烷-4-酮]体系。IV. 3,3'(1,2-亚乙基)双[2-芳基-1,3-噻唑烷-4-酮1,1-二氧化物]衍生物的合成与药理性质

3,3'-Di[1,3-thiazolidine-4-one]system. IV. Synthesis and pharmacological properties of 3,3'(1,2-ethanediyl)bis [2-aryl-1,3-thiazolidine-4-one 1,1-dioxide] derivatives.

作者信息

Vigorita M G, Previtera T, Basile M, Fenech G, Costa de Pasquale R, Occhiuto F, Circosta C

机构信息

Dipartimento Farmaco-Chimico, Facolta' di Farmacia, Universita' di Messina, Italy.

出版信息

Farmaco Sci. 1988 Apr;43(4):373-9.

PMID:3264536
Abstract

The 1,1' disulfones obtained by oxidation of the corresponding dl and meso 3,3'(1,2-ethanediyl)bis [2-aryl-4-thiazolidinone] compounds previously investigated, were evaluated as anti-histamine, anti-inflammatory, analgesic and anti-pyretic agents. All 2,2' fluorophenyl compounds were found to be significantly active in inhibiting carrageenin-induced edema, whereas only para-substituted derivatives were active on the histamine-induced bronchospasm in the guinea-pig. They also showed analgesic effects that reached and sometimes exceeded those of indomethacin and phenylbutazone used as reference drugs.

摘要

通过氧化先前研究的相应的dl和内消旋3,3'(1,2 - 乙二基)双[2 - 芳基 - 4 - 噻唑烷酮]化合物得到的1,1' - 二砜,被评估为抗组胺、抗炎、镇痛和解热剂。发现所有2,2' - 氟苯基化合物在抑制角叉菜胶诱导的水肿方面具有显著活性,而只有对位取代衍生物对豚鼠组胺诱导的支气管痉挛有活性。它们还表现出镇痛作用,达到并有时超过用作参考药物的吲哚美辛和保泰松的镇痛效果。

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