Future Microbiol 2019 02 21;14:235-245. Epub 2019 Jan 21.
Department of Chemistry, State University of Maringá, Maringá, PR, Brazil.
Aim: Novel 4-methoxy-naphthalene derivatives were synthesized based on hits structures in order to evaluate the antifungal activity against Paracoccidioides spp.
Methods: Antifungal activity of compounds was evaluated against P. brasiliensis and most promising compounds 2 and 3 were tested against eight clinically important fungal species.
Results: Compound 3 was the more active compound with MIC 8 to 32 μg.ml for Paracoccidioides spp without toxicity monkey kidney and murine macrophagecells. Carbohydrazide 3 showed good synergistic antifungal activity with amphotericin B against P. brasiliensis specie. Titration assay of carbohydrazide 3 with PbHSD enzyme demonstrates the binding ligand-protein. Molecular dynamics simulations show that ligand 3 let the PbHSD protein more stable.
Conclusion: New carbohydrazide 3 is an attractive lead for drug development to treat paracoccidioidomycoses.
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