Pecorari P, Vampa G, Rinaldi M, Melegari M, Albasini A, Provvisionato A
Farmaco Sci. 1984 Sep;39(9):781-7.
2-, 3- and 4-amino-N-(6-amino-1,4-dihydro-4-oxo-2-mercapto (or alkylthio)-5-pyrimidinyl)benzenesulfonamides were synthesized and biologically tested on different strains of Candida albicans and Candida tropicalis. Some of the 4-aminoderivatives were also tested for antibacterial properties on numerous bacterial strains. Antimycotic activity of 4-amino compounds, expressed as MIC, is around 50 micrograms/ml and higher than that of both 2-amino- and 3-aminoderivatives. In all these compounds alkyl chain length does not seem to have any notable effects on biological activity, an exception being made for some aralkyl compounds. Antibacterial activity of 4-aminoderivatives is very low for all strains tested.
合成了2-、3-和4-氨基-N-(6-氨基-1,4-二氢-4-氧代-2-巯基(或烷硫基)-5-嘧啶基)苯磺酰胺,并在白色念珠菌和热带念珠菌的不同菌株上进行了生物学测试。还对一些4-氨基衍生物在多种细菌菌株上进行了抗菌性能测试。以最低抑菌浓度(MIC)表示的4-氨基化合物的抗真菌活性约为50微克/毫升,高于2-氨基和3-氨基衍生物。在所有这些化合物中,烷基链长度似乎对生物活性没有任何显著影响,但一些芳烷基化合物除外。对于所有测试菌株,4-氨基衍生物的抗菌活性都非常低。