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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| Format: | Article |
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MDPI AG
2021-03-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/26/6/1745 |
| _version_ | 1797540616141275136 |
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| author | Roberto Romeo Salvatore V. Giofrè Maria A. Chiacchio Lucia Veltri Consuelo Celesti Daniela Iannazzo |
| author_facet | Roberto Romeo Salvatore V. Giofrè Maria A. Chiacchio Lucia Veltri Consuelo Celesti Daniela Iannazzo |
| author_sort | Roberto Romeo |
| collection | DOAJ |
| 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. |
| first_indexed | 2024-03-10T13:03:43Z |
| format | Article |
| id | doaj.art-45d36cabf5c247558fb95a8596e0012f |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T13:03:43Z |
| publishDate | 2021-03-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-45d36cabf5c247558fb95a8596e0012f2023-11-21T11:18:04ZengMDPI AGMolecules1420-30492021-03-01266174510.3390/molecules26061745Synthesis and Biological Evaluation of 2,3,4-Triaryl-1,2,4-oxadiazol-5-ones as p38 MAPK InhibitorsRoberto Romeo0Salvatore V. Giofrè1Maria A. Chiacchio2Lucia Veltri3Consuelo Celesti4Daniela Iannazzo5Dipartimento di ScienzeChimiche, Biologiche, Farmaceutiche ed Ambientali, Università di Messina, Via S.S. Annunziata, 98168 Messina, ItalyDipartimento di ScienzeChimiche, Biologiche, Farmaceutiche ed Ambientali, Università di Messina, Via S.S. Annunziata, 98168 Messina, ItalyDipartimentoScienze del Farmaco, Università di Catania, Viale A. Doria 6, 95125 Catania, ItalyDipartimento di Chimica e TecnologieChimiche, Universitàdella Calabria, Via P. Bucci 12/C, 87036 Arcavacata di Rende, ItalyDipartimento di Ingegneria, Università di Messina, Contrada Di Dio, 98166 Messina, ItalyDipartimento di Ingegneria, Università di Messina, Contrada Di Dio, 98166 Messina, ItalyA 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.https://www.mdpi.com/1420-3049/26/6/1745stilbene analogs1,2,4-oxazolidinyl-5-onesp38 MAPK inhibitors |
| spellingShingle | Roberto Romeo Salvatore V. Giofrè Maria A. Chiacchio Lucia Veltri Consuelo Celesti Daniela Iannazzo Synthesis and Biological Evaluation of 2,3,4-Triaryl-1,2,4-oxadiazol-5-ones as p38 MAPK Inhibitors Molecules stilbene analogs 1,2,4-oxazolidinyl-5-ones 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 | stilbene analogs 1,2,4-oxazolidinyl-5-ones p38 MAPK inhibitors |
| url | https://www.mdpi.com/1420-3049/26/6/1745 |
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