Research on heterocyclic compounds — Part XXXIX. 2-Methylimidazo[1,2-a]pyrimidine-3-carboxylic derivatives: Synthesis and antiinflammatory activity

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• 作者：Laneri ; Sonia ; Sacchi ; Antonia ; Gallitelli ; Marina ; Arena ; Francesca ; Luraschi ; Elena ; Abignente ; Enrico ; et. al.
• 关键词：imidazo[1 ; 2-a]pyrimidines ; antiinflammatory activity ; analgesic activity ; ulcerogenic activity ; cyclooxygenase inhibition
• 刊名：European Journal of Medicinal Chemistry
• 出版年：1998
• 出版时间：March, 1998
• 年：1998
• 卷：33
• 期：3
• 页码：163-170
• 全文大小：450 K

文摘

The synthesis of a group of 2-methylimidazo[1,2-a]pyrimidine-3-carboxylic esters, acids and amides is described. The structures of new compounds are supported by ¹H and ¹³C NMR spectra. These compounds were tested in vivo for their antiinflammatory, analgesic and ulcerogenic activity. Eight new compounds out of fifteen showed remarkable dose-dependent antiinflammatory action in the carrageenan rat paw edema (- × indomethacin) but weak analgesic activity in the acetic acid writhing test together with negligible ulcerogenic action. The new compounds were found to be lacking in inhibitory activity on cyclooxygenase in vitro.