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Thiophene-Based Compounds with Potential Anti-Inflammatory Activity

Rheumatoid arthritis, arthrosis and gout, among other chronic inflammatory diseases are public health problems and represent major therapeutic challenges. Non-steroidal anti-inflammatory drugs (NSAIDs) are the most prescribed clinical treatments, despite their severe side effects and their exclusive...

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Autores principales: da Cruz, Ryldene Marques Duarte, Mendonça-Junior, Francisco Jaime Bezerra, de Mélo, Natália Barbosa, Scotti, Luciana, de Araújo, Rodrigo Santos Aquino, de Almeida, Reinaldo Nóbrega, de Moura, Ricardo Olímpio
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8308569/
https://www.ncbi.nlm.nih.gov/pubmed/34358118
http://dx.doi.org/10.3390/ph14070692
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author da Cruz, Ryldene Marques Duarte
Mendonça-Junior, Francisco Jaime Bezerra
de Mélo, Natália Barbosa
Scotti, Luciana
de Araújo, Rodrigo Santos Aquino
de Almeida, Reinaldo Nóbrega
de Moura, Ricardo Olímpio
author_facet da Cruz, Ryldene Marques Duarte
Mendonça-Junior, Francisco Jaime Bezerra
de Mélo, Natália Barbosa
Scotti, Luciana
de Araújo, Rodrigo Santos Aquino
de Almeida, Reinaldo Nóbrega
de Moura, Ricardo Olímpio
author_sort da Cruz, Ryldene Marques Duarte
collection PubMed
description Rheumatoid arthritis, arthrosis and gout, among other chronic inflammatory diseases are public health problems and represent major therapeutic challenges. Non-steroidal anti-inflammatory drugs (NSAIDs) are the most prescribed clinical treatments, despite their severe side effects and their exclusive action in improving symptoms, without effectively promoting the cure. However, recent advances in the fields of pharmacology, medicinal chemistry, and chemoinformatics have provided valuable information and opportunities for development of new anti-inflammatory drug candidates. For drug design and discovery, thiophene derivatives are privileged structures. Thiophene-based compounds, like the commercial drugs Tinoridine and Tiaprofenic acid, are known for their anti-inflammatory properties. The present review provides an update on the role of thiophene-based derivatives in inflammation. Studies on mechanisms of action, interactions with receptors (especially against cyclooxygenase (COX) and lipoxygenase (LOX)), and structure-activity relationships are also presented and discussed. The results demonstrate the importance of thiophene-based compounds as privileged structures for the design and discovery of novel anti-inflammatory agents. The studies reveal important structural characteristics. The presence of carboxylic acids, esters, amines, and amides, as well as methyl and methoxy groups, has been frequently described, and highlights the importance of these groups for anti-inflammatory activity and biological target recognition, especially for inhibition of COX and LOX enzymes.
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spelling pubmed-83085692021-07-25 Thiophene-Based Compounds with Potential Anti-Inflammatory Activity da Cruz, Ryldene Marques Duarte Mendonça-Junior, Francisco Jaime Bezerra de Mélo, Natália Barbosa Scotti, Luciana de Araújo, Rodrigo Santos Aquino de Almeida, Reinaldo Nóbrega de Moura, Ricardo Olímpio Pharmaceuticals (Basel) Review Rheumatoid arthritis, arthrosis and gout, among other chronic inflammatory diseases are public health problems and represent major therapeutic challenges. Non-steroidal anti-inflammatory drugs (NSAIDs) are the most prescribed clinical treatments, despite their severe side effects and their exclusive action in improving symptoms, without effectively promoting the cure. However, recent advances in the fields of pharmacology, medicinal chemistry, and chemoinformatics have provided valuable information and opportunities for development of new anti-inflammatory drug candidates. For drug design and discovery, thiophene derivatives are privileged structures. Thiophene-based compounds, like the commercial drugs Tinoridine and Tiaprofenic acid, are known for their anti-inflammatory properties. The present review provides an update on the role of thiophene-based derivatives in inflammation. Studies on mechanisms of action, interactions with receptors (especially against cyclooxygenase (COX) and lipoxygenase (LOX)), and structure-activity relationships are also presented and discussed. The results demonstrate the importance of thiophene-based compounds as privileged structures for the design and discovery of novel anti-inflammatory agents. The studies reveal important structural characteristics. The presence of carboxylic acids, esters, amines, and amides, as well as methyl and methoxy groups, has been frequently described, and highlights the importance of these groups for anti-inflammatory activity and biological target recognition, especially for inhibition of COX and LOX enzymes. MDPI 2021-07-19 /pmc/articles/PMC8308569/ /pubmed/34358118 http://dx.doi.org/10.3390/ph14070692 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/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 (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
da Cruz, Ryldene Marques Duarte
Mendonça-Junior, Francisco Jaime Bezerra
de Mélo, Natália Barbosa
Scotti, Luciana
de Araújo, Rodrigo Santos Aquino
de Almeida, Reinaldo Nóbrega
de Moura, Ricardo Olímpio
Thiophene-Based Compounds with Potential Anti-Inflammatory Activity
title Thiophene-Based Compounds with Potential Anti-Inflammatory Activity
title_full Thiophene-Based Compounds with Potential Anti-Inflammatory Activity
title_fullStr Thiophene-Based Compounds with Potential Anti-Inflammatory Activity
title_full_unstemmed Thiophene-Based Compounds with Potential Anti-Inflammatory Activity
title_short Thiophene-Based Compounds with Potential Anti-Inflammatory Activity
title_sort thiophene-based compounds with potential anti-inflammatory activity
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8308569/
https://www.ncbi.nlm.nih.gov/pubmed/34358118
http://dx.doi.org/10.3390/ph14070692
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