Various 1,3,4-oxadiazole thioether 4H-chromen-4-one derivatives were conceived. The title compounds demonstrated striking inhibitory effects against Xac, Psa, and Xoo. EC50 data exhibited that A8 (19.7 μg/mL) had better antibacterial activity against Xoo than myricetin, BT, and TC. Simultaneously, the mechanism of action of A8 had been verified by SEM. The results of anti-tobacco mosaic virus indicated that A9 had the best in vivo antiviral effect compared with ningnanmycin. From the data of MST, it could be seen that A9 (0.003 ± 0.001 μmol/L) exhibited a strong binding capacity, which was far superior to ningnanmycin (2.726 ± 1.301 μmol/L). This study shows that the 1,3,4-oxadiazole thioether 4H-chromen-4-one derivatives may become agricultural drugs with great potential.

Antibacterial and Antiviral Activities of 1,3,4-Oxadiazole Thioether 4H-Chromen-4-one Derivatives.

Plant biomass is a magnificent renewable resource for phytochemicals that carry bioactive properties. Ferulic acid (FA) is a hydroxycinnamic acid that is found widespread in plant cell walls, mainly esterified to polysaccharides. It is well known of its strong antioxidant activity, together with numerous properties, such as antimicrobial, anti-inflammatory and neuroprotective effects. This review article provides insights into the potential for valorization of FA as a potent antiviral agent. Its pharmacokinetic properties (absorption, metabolism, distribution and excretion) and the proposed mechanisms that are purported to provide antiviral activity are presented. Novel strategies on extraction and derivatization routes, for enhancing even further the antiviral activity of FA and potentially favor its metabolism, distribution and residence time in the human body, are discussed. These routes may lead to novel high-added value biorefinery pathways to utilize plant biomass toward the production of nutraceuticals as functional foods with attractive bioactive properties, such as enhancing immunity toward viral infections.

https://www.frontiersin.org/articles/10.3389/fnut.2021.777576/pdf

Ferulic Acid From Plant Biomass: A Phytochemical With Promising Antiviral Properties

Antibacterial and antiviral activities and action mechanism of flavonoid derivatives with a benzimidazole moiety

Thirty-eight novel ferulic amide 1-aminocyclohexane carboxylic acid (Ac6c) derivatives D1-D19 and E1-E19 were designed and synthesized, and their antibacterial, antifungal, and insecticidal activities were tested. Most of the synthesized compounds displayed excellent activity againstXanthomonas oryzae pv. oryzae (Xoo), with EC50 values ranging from 11.6 to 83.1 μg/mL better than that of commercial bismerthiazol (BMT, EC50 = 84.3 μg/mL), as well as much better performance compared to that of thiediazole copper (TDC, EC50 = 137.8 μg/mL). D6 (EC50 = 17.3 μg/mL), D19 (EC50 = 29.4 μg/mL), E3 (EC50 = 29.7 μg/mL), E9 (EC50 = 27.0 μg/mL), E10 (EC50 = 18.6 μg/mL), and E18 (EC50 = 20.8 μg/mL) showed much higher activity on Xanthomonas oryzae pv. oryzicola compared with BMT (EC50 = 80.1 μg/mL) and TDC (EC50 = 124.7 μg/mL). In relation to controlling the fungus, Rhizoctonia solani, E1, E10, and E13 had much lower EC50 values of 0.005, 0.140, and 0.159 μg/mL compared to hymexazol at 74.8 μg/mL. Further in vivo experiments demonstrated that E6 and E12 controlled rice bacterial leaf blight disease better than BMT and TDC did. Scanning electron microscopy (SEM) studies revealed that E12 induced the Xoo cell membrane collapse. Moreover, D13 (73.7%), E5 (80.6%), and E10 (73.4%) also showed moderate activity against Plutella xylostella. These results indicated that the synthesized ferulic amide Ac6c derivatives showed promise as candidates for treating crop diseases.

Novel Ferulic Amide Ac6c Derivatives: Design, Synthesis, and Their Antipest Activity.

The novel coronavirus (nCoV) has emerged as a severe public health threat globally in the 21st century Several therapies were reported towards identifying ligand against coronavirus, including targeting specific functional proteins or enzymes that are crucial to viruses, thereby preventing the synthesis and replication of virus RNA Our study is mainly focused on targeting the virus's structural proteins, which could further block the binding of the virus to human cell receptors In our study, we have selected nine Flavonoids for the inhibition of COVID-19 Spike protein, which have already been reported with their antiviral efficacies against other virus-infected diseases AutoDock and PatchDock were used to study the inhibitory potential of flavonoids against COVID-19 Amongst all the eleven screened compounds, baicalin has depicted the highest binding affinity against 2019-nCoV spike glycoprotein Additionally, we have also compared its potential with two standard HIV drugs Abacavir and hydroxychloroquine, and the docking results clearly revealed the better inhibitory potential of baicalin in comparison to recently used drug Abacavir and hydroxychloroquine for the treatment of COVID-19 Therefore our experimental findings strongly suggested that baicalin can be used as a potential inhibitor against COVID-19 spike protein, which could inhibit the interaction of the virus with the host cell and thus could provide a potential lead molecule for the development of a drug against COVID-19 disease

/pdf/a-drug-repurposing-approach-towards-elucidating-the-2j767o1l5w.pdf

A Drug Repurposing Approach Towards Elucidating the Potential of Flavonoids as COVID-19 Spike Protein Inhibitors

A variety of myricetin derivatives bearing ferulic acid amide scaffolds were designed and synthesized. The structures of all title compounds were determined by 1H NMR, 13C NMR, 19F NMR and HRMS. Preliminary bioassays suggested that some of the target compounds exhibited remarkable antiviral activities. In particular, compound 4l possessed significant protective activity against tobacco mosaic virus (TMV), with a half maximal effective concentration (EC50) value of 196.11 μg mL−1, which was better than that of commercial agent ningnanmycin (447.92 μg mL−1). Meanwhile, microscale thermophoresis (MST) indicated that compound 4l has strong binding capability to the tobacco mosaic virus coat protein (TMV-CP) with a dissociation constant (Kd) value of 0.34 μmol L−1, which was better than that of ningnanmycin (0.52 μmol L−1). These results suggested that novel myricetin derivatives bearing ferulic acid amide scaffolds may be considered as an activator for antiviral agents.

Synthesis and antiviral activity of novel myricetin derivatives containing ferulic acid amide scaffolds

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Synthesis and antiviral activity of novel myricetin derivatives containing ferulic acid amide scaffolds