Dominika Szkatuła1, Edward Krzyżak2, Szczepan Mogilski3, Jacek Sapa3, Barbara Filipek3, Piotr Świątek1. 1. Department of Medicinal Chemistry, Faculty of Pharmacy, Wroclaw Medical University, Borowska 211, 50-556 Wroclaw, Poland. 2. Department of Inorganic Chemistry, Wrocław Medical University, ul. Borowska 211a, 50‑556 Wrocław, Poland. 3. Department of Pharmacodynamics, Faculty of Pharmacy, Jagiellonian University in Kraków, ul. Medyczna 9, 30-688 Kraków, Poland.
Abstract
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.
The subject of the work was the synthesis of new derivatives of1H-pyrrolo[3,4-c]n class="Chemical">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.
Entities:
Keywords:
3,4-pyridinedicarboximide; analgesic and sedativeactivity
Authors: Helena Sladowska; Aleksandra Sabiniarz; Dominika Szkatuła; Barbara Filipek; Jacek Sapa Journal: Acta Pol Pharm Date: 2006 Jul-Aug Impact factor: 0.330
Authors: Helena Sladowska; Barbara Filipek; Dominika Szkatuła; Aleksandra Sabiniarz; Małgorzata Kardasz; Joanna Potoczek; Maria Sieklucka-Dziuba; Grazyna Rajtar; Zdzisław Kleinrok; Tadeusz Lis Journal: Farmaco Date: 2002-11