Santos, Maria M.M.; Faria, Natália; Iley, Jim; Coles, Simon J.; Hursthouse, Michael B.; Martins, M. Luz and Moreira, Rui
Reaction of Naphthoquinones with Substituted Nitromethanes. Facile Synthesis and antifungal activity of Naphtho[2,3-d]isoxazole-4,9-diones.
Bioorganic and Medicinal Chemistry Letters, 20(1),
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We report here a simple entry into naphtho[2,3-d]isoxazole-4,9-dione system containing a EWG in position 3 using the readily available 2,3-dichloro-1,4-naphthoquinone and nitromethyl derivatives in the presence of base. Antifungal activity of synthesised naphthoquinones was evaluated against ATCC and PYCC reference strains of Candida. The results suggest that the naphtho[2,3-d]isoxazole-4,9-dione scaffold has the potential to be developed into novel and safe therapeutic antifungal agents.
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