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Bioresearch of New 1H-pyrrolo[3,4-c]pyridine-1,3(2H)-diones
Molecules ( IF 4.2 ) Pub Date : 2020-12-12 , DOI: 10.3390/molecules25245883
Dominika Szkatuła 1 , Edward Krzyżak 2 , Szczepan Mogilski 3 , Jacek Sapa 3 , Barbara Filipek 3 , Piotr Świątek 1
Affiliation  

The subject of the work was the synthesis of new derivatives of1H-pyrrolo[3,4-c]pyridine-1,3(2H)-dione with potential analgesic and sedative activity. Eight compounds werereceived. The analgesic activity of the new compounds was confirmed in the “hot plate” test and in the “writhing” test. All tested imides 8–15 were more active in the “writhing” test than aspirin, and two of them, 9 and 11, were similar to morphine. In addition, all of the new imides inhibited the locomotor activity in mice to a statistically significant extent, and two of them also prolonged the duration of thiopental sleep.On the basis of the results obtained for the previously synthesized imides and the results presented in this paper, an attempt was madeto determine the relationship between thechemical structure of imides and their analgesic and sedativeproperties.

中文翻译:

新型1H-吡咯并[3,4-c]吡啶-1,3(2H)-二酮的生物研究

该工作的主题是合成具有潜在镇痛和镇静活性的 1H-吡咯并[3,4-c]吡啶-1,3(2H)-二酮的新衍生物。收到八种化合物。在“热板”试验和“扭体”试验中证实了新化合物的镇痛活性。所有测试的酰亚胺 8-15 在“扭体”测试中都比阿司匹林更活跃,其中两个,9 和 11,与吗啡相似。此外,所有新的酰亚胺都在统计学上显着地抑制了小鼠的运动活动,其中两种还延长了硫喷妥钠的睡眠时间。该论文试图确定酰亚胺的化学结构与其镇痛和镇静特性之间的关系。
更新日期:2020-12-12
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