Cargando…

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...

Descripción completa

Detalles Bibliográficos
Autores principales: Nossier, Eman S., Fahmy, Hoda H., Khalifa, Nagy M., El-Eraky, Wafaa I., Baset, Marawan A.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2017
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
_version_ 1783357638747095040
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
work_keys_str_mv AT nossieremans designandsynthesisofnovelpyrazolesubstituteddifferentnitrogenousheterocyclicringsystemsaspotentialantiinflammatoryagents
AT fahmyhodah designandsynthesisofnovelpyrazolesubstituteddifferentnitrogenousheterocyclicringsystemsaspotentialantiinflammatoryagents
AT khalifanagym designandsynthesisofnovelpyrazolesubstituteddifferentnitrogenousheterocyclicringsystemsaspotentialantiinflammatoryagents
AT elerakywafaai designandsynthesisofnovelpyrazolesubstituteddifferentnitrogenousheterocyclicringsystemsaspotentialantiinflammatoryagents
AT basetmarawana designandsynthesisofnovelpyrazolesubstituteddifferentnitrogenousheterocyclicringsystemsaspotentialantiinflammatoryagents