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目的:研究2H-吡喃-2-酮类化合物的制备及其生物活性。方法:以乙酰乙酸乙酯为起始物,设计合成了含2H-吡喃-2-酮结构的化合物10a～10j;采用MTT法测试细胞毒活性,用ELISA法测试胆碱酯酶抑制活性。结果:合成的目标化合物及其各中间体通过1H-NMR,ESI-MS和IR确定其结构。生物活性测试中化合物10f对乙酰胆碱酯酶的IC50为6.98(10-5 mol·L-1,所有目标化合物在4.0 mg·mL-1对丁酰胆碱酯酶均无抑制作用。结论:研究发现该类化合物对乙酰胆碱酯酶有较好的选择抑制活性。
Objective: To study the preparation and biological activity of 2H-pyran-2-ones. Methods: Compounds 10a ~ 10j containing 2H-pyran-2-one were designed and synthesized using ethyl acetoacetate as starting material. The cytotoxic activity was tested by MTT assay and the inhibitory activity of cholinesterase by ELISA. Results: The structures of the synthesized target compounds and their intermediates were confirmed by1H-NMR, ESI-MS and IR. The IC50 of compound 10f for acetylcholinesterase in bioassay was 6.98 (10-5 mol·L-1), and all the target compounds showed no inhibitory effect on butyrylcholinesterase at 4.0 mg · mL-1. CONCLUSIONS: This class of compounds acetylcholinesterase better selective inhibitory activity.