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杂环化合物的研究。十四 - 咪唑并噻唑和咪唑并苯并噻唑衍生物:合成与抗炎活性。

Research on heterocyclic compounds. XIV - Imidazothiazole and imidazobenzothiazole derivatives: synthesis and antiinflammatory activity.

作者信息

Abignente E, de Caprariis P, Sacchi A, Marmo E, Berrino L, Matera M G

出版信息

Farmaco Sci. 1983 Aug;38(8):534-45. doi: 10.1002/chin.198352203.

DOI:10.1002/chin.198352203
PMID:6604663
Abstract

A group of ethyl 6-methylimidazo[2,1-b]thiazole-5-carboxylates and 2-methylimidazo[2,1-b]benzothiazole-3-carboxylates was prepared by reaction of ethyl 2-chloroacetoacetate with some 2-aminothiazoles and 2-aminobenzothiazoles, respectively. Such reactions may sometimes afford a side product which was isolated and characterized. The ethyl esters were then converted into the corresponding acids by hydrolysis. Three of these acids were evaluated for antiinflammatory, analgesic, and antipyretic activities, as well as for ulcerogenic potential.

摘要

通过使2-氯乙酰乙酸乙酯分别与一些2-氨基噻唑和2-氨基苯并噻唑反应,制备了一组6-甲基咪唑并[2,1-b]噻唑-5-羧酸乙酯和2-甲基咪唑并[2,1-b]苯并噻唑-3-羧酸乙酯。此类反应有时可能会产生一种副产物,该副产物已被分离并进行了表征。然后通过水解将乙酯转化为相应的酸。对其中三种酸进行了抗炎、镇痛和解热活性以及致溃疡潜力的评估。

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