Gershon H, Shanks L
Can J Microbiol. 1975 Sep;21(9):1317-21. doi: 10.1139/m75-198.
Twenty-one substituted 1,4-naphthoquinones and five 8-quinolinols and copper(II) chelates were tested for antifungal activity against Candida albicans and Trichophyton mentagrophytes. Compounds containing electron-releasing or weak electron-withdrawing groups in the 2 and 3 positions of the 1,4-naphthoquinone ring were the most active against C. albicans at pH 7.0 in the presence of beef serum in the following order: 2-CH3O = 2,3-(CH3O)2 greater than 2-CH3 greater than 2-CH3S greater than 2-NH2 greater than 2,6-(CH3)2. For T. mentagrophytes under the same conditions the inhibitory 1,4-naphthoquinones contained the substituents 2-CH3O greater than 2,3-(CH3O)2 greater than 2-CH2S greater than 2-CH3 greater than 2-CH3(NaHSO3) greater than 2-NH2 greater than 2-C2H5S, 3-CH3 greater than 2,6-(CH3)2 greater than 2,3-CL2 greater than 5,8-(OH)2.
测试了21种取代的1,4-萘醌、5种8-喹啉醇及其铜（II）螯合物对白色念珠菌和须癣毛癣菌的抗真菌活性。在pH 7.0且存在牛肉血清的条件下，1,4-萘醌环2位和3位含有供电子基团或弱吸电子基团的化合物对白色念珠菌的活性最高，顺序如下：2-CH3O = 2,3-(CH3O)2＞2-CH3＞2-CH3S＞2-NH2＞2,6-(CH3)2。在相同条件下，对须癣毛癣菌有抑制作用的1,4-萘醌所含取代基顺序为：2-CH3O＞2,3-(CH3O)2＞2-CH2S＞2-CH3＞2-CH3(NaHSO3)＞2-NH2＞2-C2H5S，3-CH3＞2,6-(CH3)2＞2,3-CL2＞5,8-(OH)2。
