New 4-methoxy-naphthalene derivatives as promisor antifungal agents for paracoccidioidomycosis treatment.
Future Microbiol
; 14: 235-245, 2019 02.
Article
en En
| MEDLINE
| ID: mdl-30663901
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.Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Paracoccidioides
/
Paracoccidioidomicosis
/
Antifúngicos
/
Naftalenos
Límite:
Animals
Idioma:
En
Revista:
Future Microbiol
Asunto de la revista:
MICROBIOLOGIA
Año:
2019
Tipo del documento:
Article
País de afiliación:
Brasil