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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...

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Detalles Bibliográficos
Autores principales: Said Fatahala, Samar, Hasabelnaby, Sherifa, Goudah, Ayman, Mahmoud, Ghada I., Helmy Abd-El Hameed, Rania
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2017
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.
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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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