i-Med.UL, Faculdade de Farmácia, Universidade de Lisboa, Av. Forças Armadas, Lisboa, Portugal.
Bioorg Med Chem Lett. 2010 Jan 1;20(1):193-5. doi: 10.1016/j.bmcl.2009.10.137. Epub 2009 Nov 4.
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.
我们在这里报道了一种简单的方法，可在碱的存在下，利用易得的 2,3-二氯-1,4-萘醌和硝甲基衍生物，在 3 位引入含有吸电子基团（EWG）的萘并[2,3-d]异恶唑-4,9-二酮系统。合成的萘醌类化合物的抗真菌活性已针对 ATCC 和 PYCC 参考株的念珠菌进行了评估。结果表明，萘并[2,3-d]异恶唑-4,9-二酮支架有可能被开发成新型、安全的抗真菌治疗药物。
