Mannich bases of 5-hydroxynaphthalene-1,8-carbolactone 1 were prepared from various secondary amines or bulky primary amines and formaldehyde. They were isolated in almost all cases as hydrochlorides. These derivatives were submitted to in vitro antifungal and cytotoxic assays. The antifungal assays were performed against three strains of yeasts and five strains of human pathogenic fungi. Two of the tested compounds, 2i and 2j, exhibited interesting antifungal activities against Candida albicans and Candida tropicalis. The cytotoxic activity was evaluated towards L 1210 leukemia cells. Almost all of the Mannich bases had shown significant activity against this tumor cell line as values of IC50 less than or equal to 4 micrograms/ml are considered interesting. Only one derivative 2 developed better cytotoxicity than the parent compound 1.

中文翻译：

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5-羟基萘-1,8-碳内酯曼尼希碱的合成作为潜在的抗真菌剂或抗肿瘤剂。

5-羟基萘-1,8-碳内酯1的曼尼希碱是由各种仲胺或庞大的伯胺和甲醛制备的。在几乎所有情况下，它们都被分离为盐酸盐。这些衍生物已进行了体外抗真菌和细胞毒性试验。针对三株酵母和五株人病原性真菌进行了抗真菌测定。两种测试化合物2i和2j对白念珠菌和热带念珠菌表现出有趣的抗真菌活性。评价了对L 1210白血病细胞的细胞毒活性。几乎所有的曼尼希碱都显示出对这种肿瘤细胞系的显着活性，因为IC50值小于或等于4微克/毫升被认为是令人感兴趣的。只有一种衍生物2具有比母体化合物1更好的细胞毒性。