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以2,4-二氨基-6-羟甲基吡啶并[3,2-d]嘧啶为原料,在4-位氨基转换为羟基后与对氨基苯甲酰谷氨酸二乙酯连接生成叶酸类似物分子骨架,采用Adams催化方法还原吡啶环,在N5-位连接不同类型的取代基得到3个新的N8-去氮四氢叶酸类似物.经1H NMR,MS对化合物的结构进行了表征.初步生物活性结果表明,此类化合物对人重组二氢叶酸还原酶的抑制活性与N5-位的取代基有关联.
Using 2,4-diamino-6-hydroxymethylpyrido [3,2-d] pyrimidine as starting material, folic acid was formed by the conversion of the amino group at the 4-position to the hydroxyl group upon coupling with diethyl-aminobenzoyl glutamate Analogs backbone, using Adams catalytic reduction of pyridine ring, N5-position to connect different types of substituents to obtain three new N8-deaza tetrahydrofolate analogues by 1H NMR, MS compound structure was characterized Preliminary bioactivity results indicate that the inhibitory activity of such compounds on human recombinant dihydrofolate reductase is associated with a substituent at the N5-position.