Antibacterial, antifungal, and antiviral activities of chalcone-bearing tetrahydropyranyl and 2, 4-dihydroxyl moieties

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Abstract

Chalcones highlights as an important structure in medicinal chemistry and thus has been widely used as a template in the development of new drugs. In this study, we aim to determine the antibacterial, anti-Candida, and anti-Dengue potential of new chalcone-bearing 2, 4-dihydroxyl and tetrahydropyranyl moieties. Antimicrobial activity assays showed that microorganism of the Staphylococcus genus (including methicillin-resistant strains) were susceptible to 2, 4-dihydroxychalcones, with minimum inhibitory concentrations (MICs) ranging of 19.5 to 125 µg.mL-1. Compound 4e, which showed the highest bacteriostatic effect, also has bactericidal activity from of 80 µg.mL-1. The growth of oral isolates of Candida albicans was also efficiently inhibited with compound 4e (MIC: 15.6–32.3 µg.mL-1), which was fungicidal at 15.6 µg.mL-1. However, the presence of the tetrahydropyranyl moiety impaired both the antibacterial and antifungal effects. None of the chalcones tested were actives against Dengue virus serotype 2. In conclusion, the compound 4e showed good anti-Staphylococci and anti-Candida activity and may be a promising prototype for the development of new antimicrobial agents.

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Lima, W. G., Andrade, J. T., da Silva Santos, F. R., Palumbo, J. M. C., Herrera, K. M. S., de Castro, L. E., … Ferreira, J. M. S. (2020). Antibacterial, antifungal, and antiviral activities of chalcone-bearing tetrahydropyranyl and 2, 4-dihydroxyl moieties. Revista Colombiana de Ciencias Quimico-Farmaceuticas(Colombia), 49(1), 218–233. https://doi.org/10.15446/RCCIQUIFA.V49N1.87036

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