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Bioresearch of New 1H-pyrrolo[3,4-c]pyridine-1,3(2H)-diones
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 teste...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2020
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7764601/ https://www.ncbi.nlm.nih.gov/pubmed/33322767 http://dx.doi.org/10.3390/molecules25245883 |
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author | Szkatuła, Dominika Krzyżak, Edward Mogilski, Szczepan Sapa, Jacek Filipek, Barbara Świątek, Piotr |
author_facet | Szkatuła, Dominika Krzyżak, Edward Mogilski, Szczepan Sapa, Jacek Filipek, Barbara Świątek, Piotr |
author_sort | Szkatuła, Dominika |
collection | PubMed |
description | 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. |
format | Online Article Text |
id | pubmed-7764601 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-77646012020-12-27 Bioresearch of New 1H-pyrrolo[3,4-c]pyridine-1,3(2H)-diones Szkatuła, Dominika Krzyżak, Edward Mogilski, Szczepan Sapa, Jacek Filipek, Barbara Świątek, Piotr Molecules Article 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. MDPI 2020-12-12 /pmc/articles/PMC7764601/ /pubmed/33322767 http://dx.doi.org/10.3390/molecules25245883 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Szkatuła, Dominika Krzyżak, Edward Mogilski, Szczepan Sapa, Jacek Filipek, Barbara Świątek, Piotr Bioresearch of New 1H-pyrrolo[3,4-c]pyridine-1,3(2H)-diones |
title | Bioresearch of New 1H-pyrrolo[3,4-c]pyridine-1,3(2H)-diones |
title_full | Bioresearch of New 1H-pyrrolo[3,4-c]pyridine-1,3(2H)-diones |
title_fullStr | Bioresearch of New 1H-pyrrolo[3,4-c]pyridine-1,3(2H)-diones |
title_full_unstemmed | Bioresearch of New 1H-pyrrolo[3,4-c]pyridine-1,3(2H)-diones |
title_short | Bioresearch of New 1H-pyrrolo[3,4-c]pyridine-1,3(2H)-diones |
title_sort | bioresearch of new 1h-pyrrolo[3,4-c]pyridine-1,3(2h)-diones |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7764601/ https://www.ncbi.nlm.nih.gov/pubmed/33322767 http://dx.doi.org/10.3390/molecules25245883 |
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