Synthesis and Biological Evaluation of 2,3,4-Triaryl-1,2,4-oxadiazol-5-ones as p38 MAPK Inhibitors

A series of azastilbene derivatives, characterized by the presence of the 1,2,4-oxadiazole-5-one system as a linker of the two aromatic rings of stilbenes, have been prepared as novel potential inhibitors of p38 MAPK. Biological assays indicated that some of the synthesized compounds are endowed wit...

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Autores principales: Romeo, Roberto, Giofrè, Salvatore V., Chiacchio, Maria A., Veltri, Lucia, Celesti, Consuelo, Iannazzo, Daniela
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8003627/
https://www.ncbi.nlm.nih.gov/pubmed/33804659
http://dx.doi.org/10.3390/molecules26061745
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author Romeo, Roberto
Giofrè, Salvatore V.
Chiacchio, Maria A.
Veltri, Lucia
Celesti, Consuelo
Iannazzo, Daniela
author_facet Romeo, Roberto
Giofrè, Salvatore V.
Chiacchio, Maria A.
Veltri, Lucia
Celesti, Consuelo
Iannazzo, Daniela
author_sort Romeo, Roberto
collection PubMed
description A series of azastilbene derivatives, characterized by the presence of the 1,2,4-oxadiazole-5-one system as a linker of the two aromatic rings of stilbenes, have been prepared as novel potential inhibitors of p38 MAPK. Biological assays indicated that some of the synthesized compounds are endowed with good inhibitory activity towards the kinase. Molecular modeling data support the biological results showing that the designed compounds possess a reasonable binding mode in the ATP binding pocket of p38α kinase with a good binding affinity.
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spelling pubmed-80036272021-03-28 Synthesis and Biological Evaluation of 2,3,4-Triaryl-1,2,4-oxadiazol-5-ones as p38 MAPK Inhibitors Romeo, Roberto Giofrè, Salvatore V. Chiacchio, Maria A. Veltri, Lucia Celesti, Consuelo Iannazzo, Daniela Molecules Article A series of azastilbene derivatives, characterized by the presence of the 1,2,4-oxadiazole-5-one system as a linker of the two aromatic rings of stilbenes, have been prepared as novel potential inhibitors of p38 MAPK. Biological assays indicated that some of the synthesized compounds are endowed with good inhibitory activity towards the kinase. Molecular modeling data support the biological results showing that the designed compounds possess a reasonable binding mode in the ATP binding pocket of p38α kinase with a good binding affinity. MDPI 2021-03-20 /pmc/articles/PMC8003627/ /pubmed/33804659 http://dx.doi.org/10.3390/molecules26061745 Text en © 2021 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
Romeo, Roberto
Giofrè, Salvatore V.
Chiacchio, Maria A.
Veltri, Lucia
Celesti, Consuelo
Iannazzo, Daniela
Synthesis and Biological Evaluation of 2,3,4-Triaryl-1,2,4-oxadiazol-5-ones as p38 MAPK Inhibitors
title Synthesis and Biological Evaluation of 2,3,4-Triaryl-1,2,4-oxadiazol-5-ones as p38 MAPK Inhibitors
title_full Synthesis and Biological Evaluation of 2,3,4-Triaryl-1,2,4-oxadiazol-5-ones as p38 MAPK Inhibitors
title_fullStr Synthesis and Biological Evaluation of 2,3,4-Triaryl-1,2,4-oxadiazol-5-ones as p38 MAPK Inhibitors
title_full_unstemmed Synthesis and Biological Evaluation of 2,3,4-Triaryl-1,2,4-oxadiazol-5-ones as p38 MAPK Inhibitors
title_short Synthesis and Biological Evaluation of 2,3,4-Triaryl-1,2,4-oxadiazol-5-ones as p38 MAPK Inhibitors
title_sort synthesis and biological evaluation of 2,3,4-triaryl-1,2,4-oxadiazol-5-ones as p38 mapk inhibitors
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8003627/
https://www.ncbi.nlm.nih.gov/pubmed/33804659
http://dx.doi.org/10.3390/molecules26061745
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