A new and suitable multicomponent one-pot reaction was developed for the synthesis of 2-amino-3-cyanopyridine derivatives. Background: This synthesis was demonstrated by the efficient and easy access to a variety of substituted 2-aminopyridines using enaminones as key precursors under solvent-free conditions. Methods: A range of spectroscopic techniques was used to determine and confirm the chemical structures (FTIR, 1H NMR, 13C NMR). The antimicrobial potency of synthesized compounds (2a–d) was tested using disk diffusion assays, and the Minimum Inhibitory Concentration (MIC) for the active compounds was determined against a panel of microorganisms, including Gram-positive and Gram-negative bacteria and yeasts. Moreover, a docking analysis was conducted by Molecular Operating Environment (MOE) software to provide supplementary information about the potential, as well as an ADME-T prediction to describe the pharmacokinetic properties of the best compound and its toxicity. Results: The results of the antimicrobial activity indicated that compound 2c showed the highest activity against Gram-positive bacteria, particularly S. aureus and B. subtilis whose MIC values were 0.039 ± 0.000 µg·mL−1. The results of the theoretical study of compound 2c were in line with the experimental data and exhibited excellent antibacterial potential. Conclusions: On the basis of the obtained results, compound 2c can be used as an antibacterial agent model with high antibacterial potency.
Honey is a complex natural nutrient with well-established therapeutic properties recognized in traditional medicine. The purpose of the current work was to compare, in vitro, the bioactive compounds, antioxidants, and antimicrobial properties of 37 honey samples collected from the western region of Algeria and to identify the best sample for potential therapeutic purposes. Estimation of bioactive compounds was carried out by determining the total phenolic and flavonoid contents. Large variability among the samples was observed regarding the total phenolic content (from 24.17 ± 1.38 to 122.15 ± 3.55 mg GAE/100 g honey) and total flavonoid content (from 0.07 ± 0.01 to 33.49 ± 4.90 mg QE/100 g honey). Additionally, antioxidant activity, evaluated by four spectrophotometric assays, displayed fluctuating results among the samples. High positive correlations were observed between β-carotene and DPPH (0.766) and between β-carotene and ABTS (0.600), while inverse correlations were observed between bioactive compounds and antioxidant activity, except for the FRAP method. The antimicrobial activity, determined by well-diffusion assays, exhibited a dose-dependent antibacterial effect, with significant inhibition toward methicillin-resistant Staphylococcus aureus and Pseudomonas aeruginosa reference strains. However, no activity was observed against Candida albicans strains. The MIC and MBC values were identical in most samples (range: 60 to 80% w/v) and predominantly exhibited bactericidal effects. The content of bioactive compounds played a significant role in the antibacterial properties. To summarize, the best honey sample for potential therapeutic purposes corresponded to mild white mustard (S6) and might be used as an alternative in therapeutic applications.
A convenient and effective synthesis of imidazo[1,2-a]pyrimidine derivatives has been developed under microwave irradiations using Al2O3 as a catalyst in solvent-free conditions. The functionalized imidazo[1,2-a]pyrimidine derivatives are useful in biochemistry and medical science. In our investigation, the antimicrobial activity of the synthesized compounds was evaluated against 13 microorganisms, including 6 Gram-positive bacteria, 4 Gram-negative bacteria, and 3 pathogenic fungi. Bioactivity tests revealed that the majority of the compounds exhibited good antimicrobial activity. Finally, molecular docking simulations and ADME-T predictions were performed, showing that the most active compounds have good binding modes with microbial targets and promising pharmacokinetic safety profiles.
Honey, beyond its nutritional and therapeutic value, can act as a natural bioindicator of environmental quality. In this study, fourteen unifloral and multifloral honeys from northern Algeria were analysed for toxic metals using atomic absorption spectrometry and inductively coupled plasma mass spectrometry. Concentrations were as follows: Cu (0.133–1.975 µg/kg), Fe (1.11–28.04 mg/kg), Zn (4.40–26.30 mg/kg), Cd (1.119–39.521 µg/kg), and Pb (11.515–77.216 µg/kg). Some samples, particularly for Cd and Pb, exceeded international safety limits, indicating potential health risks. The results confirm the importance of routine monitoring and highlight honey’s relevance in food safety and environmental surveillance.
Natural honey is a widely consumed product in various cultures. Owing to the foraging behaviour of bees and the unique production process of honey, this matrix serves as a critical tool for environmental biomonitoring. The aim of this study was to assess the content of selected toxic elements, specifically cadmium (Cd), lead (Pb), arsenic (As), and mercury (Hg), in honeys from Poland and Algeria. Additionally, the existence of health risks associated with long-term consumption was assessed. The As, Cd, and Pb content was determined using ICP-MS after prior microwave digestion of the samples in a closed system. Hg content was determined directly using the AAS method with the amalgamation technique. A total of 41 honey samples from Algeria and Poland were analysed. The content of the tested toxic elements in most samples was low. The results obtained for Pb were compared to applicable standards; exceedances for Pb were observed in 7% of the samples. Despite this, the estimated exposure did not indicate a significant health risk to consumers. The above data indicate that honey is not only a valuable nutritional product but also represents an important bioindicator of environmental pollution.