Back to Search
Start Over
Synthesis and Biological Evaluation of 2,3,4-Triaryl-1,2,4-oxadiazol-5-ones as p38 MAPK Inhibitors
- Source :
- Molecules, Vol 26, Iss 1745, p 1745 (2021), Molecules, Volume 26, Issue 6
- Publication Year :
- 2021
- Publisher :
- MDPI AG, 2021.
-
Abstract
- 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.
- Subjects :
- Molecular model
Stereochemistry
p38 mitogen-activated protein kinases
Drug Evaluation, Preclinical
Pharmaceutical Science
p38 MAPK inhibitors
Molecular Docking Simulation
p38 Mitogen-Activated Protein Kinases
Article
Analytical Chemistry
4-oxazolidinyl-5-ones
lcsh:QD241-441
03 medical and health sciences
Structure-Activity Relationship
0302 clinical medicine
lcsh:Organic chemistry
Drug Discovery
Structure–activity relationship
Humans
stilbene analogs
Physical and Theoretical Chemistry
Protein Kinase Inhibitors
030304 developmental biology
Biological evaluation
0303 health sciences
1,2,4-oxazolidinyl-5-ones
Kinase
Chemistry
Organic Chemistry
Aromaticity
Chemistry (miscellaneous)
030220 oncology & carcinogenesis
Drug Design
Molecular Medicine
Linker
Subjects
Details
- Language :
- English
- ISSN :
- 14203049
- Volume :
- 26
- Issue :
- 1745
- Database :
- OpenAIRE
- Journal :
- Molecules
- Accession number :
- edsair.doi.dedup.....fdc3dca1b2ae8af58dd3898e5e8bcbbc