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.

Il Farmaco; edizione scientifica Pub Date : 1988-04-01
M G Vigorita, T Previtera, M Basile, G Fenech, R Costa de Pasquale, F Occhiuto, C Circosta
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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.

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3, 3 ' di (1, 3-thiazolidine-4-one)系统。3,3'(1,2-乙二基)双[2-芳基-1,3-噻唑烷-4- 1,1-二氧基]衍生物的合成和药理学性质。
通过氧化相应的dl和中位3,3'(1,2-乙二基)双[2-芳基-4-噻唑烷酮]化合物得到的1,1'二砜类化合物被评价为抗组胺、抗炎、镇痛和抗热药物。所有2,2'氟苯基化合物都能显著抑制卡拉胶素诱导的水肿,而只有准取代衍生物对组胺诱导的豚鼠支气管痉挛有活性。它们的镇痛效果达到甚至有时超过了作为对照药的吲哚美辛和苯丁酮。
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