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Pyrrole and Fused Pyrrole Compounds with Bioactivity against Inflammatory Mediators
A new series of pyrrolopyridines and pyrrolopyridopyrimidines have been synthesized from aminocyanopyrroles. The synthesized compounds have been characterized by FTIR, (1)H-NMR and mass spectroscopy. The final compounds have been screened for in vitro pro-inflammatory cytokine inhibitory and in vivo...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2017
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6155178/ https://www.ncbi.nlm.nih.gov/pubmed/28304349 http://dx.doi.org/10.3390/molecules22030461 |
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author | Said Fatahala, Samar Hasabelnaby, Sherifa Goudah, Ayman Mahmoud, Ghada I. Helmy Abd-El Hameed, Rania |
author_facet | Said Fatahala, Samar Hasabelnaby, Sherifa Goudah, Ayman Mahmoud, Ghada I. Helmy Abd-El Hameed, Rania |
author_sort | Said Fatahala, Samar |
collection | PubMed |
description | A new series of pyrrolopyridines and pyrrolopyridopyrimidines have been synthesized from aminocyanopyrroles. The synthesized compounds have been characterized by FTIR, (1)H-NMR and mass spectroscopy. The final compounds have been screened for in vitro pro-inflammatory cytokine inhibitory and in vivo anti-inflammatory activity. The biological results revealed that among all tested compounds some fused pyrroles, namely the pyrrolopyridines 3i and 3l, show promising activity. A docking study of the active synthesized molecules confirmed the biological results and revealed a new binding pose in the COX-2 binding site. |
format | Online Article Text |
id | pubmed-6155178 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2017 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-61551782018-11-13 Pyrrole and Fused Pyrrole Compounds with Bioactivity against Inflammatory Mediators Said Fatahala, Samar Hasabelnaby, Sherifa Goudah, Ayman Mahmoud, Ghada I. Helmy Abd-El Hameed, Rania Molecules Article A new series of pyrrolopyridines and pyrrolopyridopyrimidines have been synthesized from aminocyanopyrroles. The synthesized compounds have been characterized by FTIR, (1)H-NMR and mass spectroscopy. The final compounds have been screened for in vitro pro-inflammatory cytokine inhibitory and in vivo anti-inflammatory activity. The biological results revealed that among all tested compounds some fused pyrroles, namely the pyrrolopyridines 3i and 3l, show promising activity. A docking study of the active synthesized molecules confirmed the biological results and revealed a new binding pose in the COX-2 binding site. MDPI 2017-03-17 /pmc/articles/PMC6155178/ /pubmed/28304349 http://dx.doi.org/10.3390/molecules22030461 Text en © 2017 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 Said Fatahala, Samar Hasabelnaby, Sherifa Goudah, Ayman Mahmoud, Ghada I. Helmy Abd-El Hameed, Rania Pyrrole and Fused Pyrrole Compounds with Bioactivity against Inflammatory Mediators |
title | Pyrrole and Fused Pyrrole Compounds with Bioactivity against Inflammatory Mediators |
title_full | Pyrrole and Fused Pyrrole Compounds with Bioactivity against Inflammatory Mediators |
title_fullStr | Pyrrole and Fused Pyrrole Compounds with Bioactivity against Inflammatory Mediators |
title_full_unstemmed | Pyrrole and Fused Pyrrole Compounds with Bioactivity against Inflammatory Mediators |
title_short | Pyrrole and Fused Pyrrole Compounds with Bioactivity against Inflammatory Mediators |
title_sort | pyrrole and fused pyrrole compounds with bioactivity against inflammatory mediators |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6155178/ https://www.ncbi.nlm.nih.gov/pubmed/28304349 http://dx.doi.org/10.3390/molecules22030461 |
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