期刊
FUTURE MICROBIOLOGY
卷 14, 期 3, 页码 235-246出版社
FUTURE MEDICINE LTD
DOI: 10.2217/fmb-2018-0276
关键词
antifungal activity; carbohydrazide; homoserine dehydrogenase; molecular modeling
类别
资金
- Coordenacao de Aperfeicoamento de Pessoal de NivelSuperior (CAPES)
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 32g.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.
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