为了探索天然产物Cedarmycins衍生物的结构与活性关系,以α-亚甲基-β-羟甲基-γ-丁内酯为起始原料,经过与不同取代的羧酸缩合,合成了19个新的(4-亚甲基-5-羰基-3-四氢呋喃基)-苯甲酸甲酯衍生物。杀菌活性测定结果表明,该类衍生物具有广谱的杀菌活性,尤其对水稻纹枯病菌Rhizoctonia solani和辣椒疫霉Phytophthora capsici显示出很强的杀菌活性,其中化合物2e(R=2,4-2Cl)对这2种病菌的EC50值约为1.6 mg/L。
In order to elucidate structure-activity relationship of natural product Cedarmycins, a series of novel ( 4-methylene-5-oxo-tetrahydrofuran-3-yl ) methyl benzoate derivatives ( 2a-2s ) were synthesized by condensation of 4-(hydroxymethyl)-5-methylene-dihydrofuran-2(3H)-one with various substituted benzoate acids. The preliminary bioassay showed that some of these compounds have good fungicidal activity, especially against Rhizoctonia solani and Phytophthora capsici. The EC50 value of compound 2e( R =2,4-2Cl) were about 1.6 mg/L for the above fungus.