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- W2913663145 abstract "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 -1 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." @default.
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- W2913663145 date "2019-02-01" @default.
- W2913663145 modified "2023-10-12" @default.
- W2913663145 title "New 4-methoxy-naphthalene derivatives as promisor antifungal agents for paracoccidioidomycosis treatment" @default.
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- W2913663145 doi "https://doi.org/10.2217/fmb-2018-0276" @default.
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