若干莽草酸衍生物的合成和生物活性研究

STUDIES ON THE SYNTHESIS AND BIOACTIVITY OF SOME NEW SHIKIMIC ACID DERIVATIVES

虽然对莽草酸(shikimic acid)的研究由来已久,但只是在陆续发现了具有生物活性的乙二醛酶Ⅰ抑制剂(glyoxalase Ⅰinhibitor 1)和二(口恶)霉素(dioxolamycin 2)等含莽草酸类母核的天然产物后,才有合成莽草酸衍生物进行生物活性研究的报道,即由莽草酸甲酯合成乙二醛酶Ⅰ抑制剂的类似物3。

Ten new shikimic acid derivatives, some of which are analogs of dioxolamycin were synthesized from methyl Shikimate because the bioactivity of shikimic acid derivatives has received considerably less attention to date. Compounds 4～10, 12, 16 were subjected to antimicrobial test in vitro, and showed no activity (MIC>25 μ/ml ). Compounds 4～10, 12, 13, and 16 were subjected to cytostatic activity test against cultured , L 1210 Leukemia cells in vitro. Compounds 4, 6, 13 and 16 showed cytostatic activity like dioxolamycin.