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Design and Synthesis of Novel Pyrazole-Substituted Different Nitrogenous Heterocyclic Ring Systems as Potential Anti-Inflammatory Agents
With the aim of developing novel anti-inflammatory scaffolds, a new series of pyrazole-substituted various nitrogenous heterocyclic ring systems at C-4 position were synthesized through different chemical reactions and validated by means of spectral and elemental data. The new obtained compounds wer...
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/PMC6154115/ https://www.ncbi.nlm.nih.gov/pubmed/28338602 http://dx.doi.org/10.3390/molecules22040512 |
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author | Nossier, Eman S. Fahmy, Hoda H. Khalifa, Nagy M. El-Eraky, Wafaa I. Baset, Marawan A. |
author_facet | Nossier, Eman S. Fahmy, Hoda H. Khalifa, Nagy M. El-Eraky, Wafaa I. Baset, Marawan A. |
author_sort | Nossier, Eman S. |
collection | PubMed |
description | With the aim of developing novel anti-inflammatory scaffolds, a new series of pyrazole-substituted various nitrogenous heterocyclic ring systems at C-4 position were synthesized through different chemical reactions and validated by means of spectral and elemental data. The new obtained compounds were investigated for their anti-inflammatory activity using the carrageenan-induced paw edema standard technique and revealed that, compound 6b showed increased potency with % inhibition of edema 85.23 ± 1.92 and 85.78 ± 0.99, respectively, higher than the standard reference drugs indomethacin and celebrex (72.99% and 83.76%). Molecular modeling studies were initiated herein to validate the attained pharmacological data and provide understandable evidence for the observed anti-inflammatory behavior. |
format | Online Article Text |
id | pubmed-6154115 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2017 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-61541152018-11-13 Design and Synthesis of Novel Pyrazole-Substituted Different Nitrogenous Heterocyclic Ring Systems as Potential Anti-Inflammatory Agents Nossier, Eman S. Fahmy, Hoda H. Khalifa, Nagy M. El-Eraky, Wafaa I. Baset, Marawan A. Molecules Article With the aim of developing novel anti-inflammatory scaffolds, a new series of pyrazole-substituted various nitrogenous heterocyclic ring systems at C-4 position were synthesized through different chemical reactions and validated by means of spectral and elemental data. The new obtained compounds were investigated for their anti-inflammatory activity using the carrageenan-induced paw edema standard technique and revealed that, compound 6b showed increased potency with % inhibition of edema 85.23 ± 1.92 and 85.78 ± 0.99, respectively, higher than the standard reference drugs indomethacin and celebrex (72.99% and 83.76%). Molecular modeling studies were initiated herein to validate the attained pharmacological data and provide understandable evidence for the observed anti-inflammatory behavior. MDPI 2017-03-24 /pmc/articles/PMC6154115/ /pubmed/28338602 http://dx.doi.org/10.3390/molecules22040512 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 Nossier, Eman S. Fahmy, Hoda H. Khalifa, Nagy M. El-Eraky, Wafaa I. Baset, Marawan A. Design and Synthesis of Novel Pyrazole-Substituted Different Nitrogenous Heterocyclic Ring Systems as Potential Anti-Inflammatory Agents |
title | Design and Synthesis of Novel Pyrazole-Substituted Different Nitrogenous Heterocyclic Ring Systems as Potential Anti-Inflammatory Agents |
title_full | Design and Synthesis of Novel Pyrazole-Substituted Different Nitrogenous Heterocyclic Ring Systems as Potential Anti-Inflammatory Agents |
title_fullStr | Design and Synthesis of Novel Pyrazole-Substituted Different Nitrogenous Heterocyclic Ring Systems as Potential Anti-Inflammatory Agents |
title_full_unstemmed | Design and Synthesis of Novel Pyrazole-Substituted Different Nitrogenous Heterocyclic Ring Systems as Potential Anti-Inflammatory Agents |
title_short | Design and Synthesis of Novel Pyrazole-Substituted Different Nitrogenous Heterocyclic Ring Systems as Potential Anti-Inflammatory Agents |
title_sort | design and synthesis of novel pyrazole-substituted different nitrogenous heterocyclic ring systems as potential anti-inflammatory agents |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6154115/ https://www.ncbi.nlm.nih.gov/pubmed/28338602 http://dx.doi.org/10.3390/molecules22040512 |
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