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Bioassay of ferulic acid derivatives as influenza neuraminidase inhibitors
- Source :
- Archiv der Pharmazie. 353:1900174
- Publication Year :
- 2019
- Publisher :
- Wiley, 2019.
-
Abstract
- Four series of ferulic acid derivatives were designed, synthesized, and evaluated for their neuraminidase (NA) inhibitory activities against influenza virus H1N1 in vitro. The pharmacological results showed that the majority of the target compounds exhibited moderate influenza NA inhibitory activity, which was also better than that of ferulic acid. The two most potent compounds were 1m and 4a with IC50 values of 12.77 ± 0.47 and 12.96 ± 1.34 μg/ml, respectively. On the basis of the biological results, a preliminary structure-activity relationship (SAR) was derived and discussed. Besides, molecular docking was performed to study the possible interactions of compounds 1p, 2d, 3b, and 4a with the active site of NA. It was found that the 4-OH-3-OMe group and the amide group (CON) of ferulic acid amide derivatives were two key pharmacophores for NA inhibitory activity. It is meaningful to further modify the natural product ferulic acid to improve its influenza NA inhibitory activity.
- Subjects :
- Models, Molecular
Coumaric Acids
Stereochemistry
Neuraminidase
Pharmaceutical Science
Microbial Sensitivity Tests
Crystallography, X-Ray
Antiviral Agents
01 natural sciences
Ferulic acid
Structure-Activity Relationship
chemistry.chemical_compound
Influenza A Virus, H1N1 Subtype
Amide
Drug Discovery
Humans
Bioassay
Enzyme Inhibitors
Natural product
Dose-Response Relationship, Drug
Molecular Structure
biology
010405 organic chemistry
Chemistry
Active site
In vitro
0104 chemical sciences
010404 medicinal & biomolecular chemistry
biology.protein
Biological Assay
Pharmacophore
Subjects
Details
- ISSN :
- 15214184 and 03656233
- Volume :
- 353
- Database :
- OpenAIRE
- Journal :
- Archiv der Pharmazie
- Accession number :
- edsair.doi.dedup.....61aa1bd5e9d51b5f3c2de1bd034bf1d1