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4-烷氧基-6-甲基-1H-吡咯并[3,4-c]吡啶-1,3(2H)-二酮的N-取代衍生物的合成及药理性质研究

Investigations on the synthesis and pharmacological properties of N-substituted derivatives of 4-alkoxy-6-methyl-1H-pyrrolo[3,4-c]pyridine-1,3(2H)-diones.

作者信息

Sladowska Helena, Filipek Barbara, Szkatuła Dominika, Sapa Jacek, Bednarski Marek, Ciołkowska Marta

机构信息

Department of Chemistry of Drugs, Wrocław University of Medicine, Tamka 1, 50-137 Wrocław, Poland.

出版信息

Farmaco. 2005 Jan;60(1):53-9. doi: 10.1016/j.farmac.2004.08.011. Epub 2004 Dec 19.

Abstract

Synthesis of N-substituted derivatives of 4-alkoxy-6-methyl-1H-pyrrolo[3,4-c]pyridine-1,3(2H)-diones (10-14, 18-21) is described. In the "writhing syndrome" test all compounds studied exhibited potent analgesic activity which was superior than that of acetylsalicylic acid. In the "hot plate" test imides 10, 12, 13, 18-20 acted also stronger than aspirin. Furthermore all compounds tested significantly suppressed the spontaneous locomotor activity of mice and prolonged barbiturate sleep of these animals.

摘要

描述了4-烷氧基-6-甲基-1H-吡咯并[3,4-c]吡啶-1,3(2H)-二酮(10-14、18-21)的N-取代衍生物的合成。在“扭体综合征”试验中,所有研究的化合物均表现出强效镇痛活性,优于乙酰水杨酸。在“热板”试验中,酰亚胺10、12、13、18-20的作用也比阿司匹林更强。此外,所有测试化合物均显著抑制小鼠的自发运动活性,并延长这些动物的巴比妥类睡眠时间。

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