Reaction of naphthoquinones with substituted nitromethanes. Facile synthesis and antifungal activity of naphtho[2,3-d]isoxazole-4,9-diones |
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| Authors: | Maria MM Santos Natália Faria Jim Iley Simon J Coles Michael B Hursthouse M Luz Martins Rui Moreira |
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| Institution: | 1. i-Med.UL, Faculdade de Farmácia, Universidade de Lisboa, Av. Forças Armadas, Lisboa, Portugal;2. Mycology Laboratory, IHMT/CREM, New University of Lisbon, Lisboa, Portugal;3. Chemistry Department, The Open University, Milton Keynes, UK;4. EPSRC National Crystallography Service, School of Chemistry, University of Southampton, Southampton, UK |
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| Abstract: | We report here a simple entry into naphtho2,3-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 naphtho2,3-d]isoxazole-4,9-dione scaffold has the potential to be developed into novel and safe therapeutic antifungal agents. |
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