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以邻苯二胺和乙酰乙酸乙酯为起始原料制得异丙烯基苯并咪唑酮(Ⅲ),再经N-酰化反应得到13个苯并咪唑酮酰胺衍生物(Ⅳ-01～Ⅳ-13)以及由Ⅳ-02脱异丙烯基的产物Ⅳ-02a,其中9个为未见文献报道的新化合物。通过核磁共振氢谱和碳谱、质谱以及元素分析对其结构进行了表征。抑菌活性测定结果表明,化合物Ⅳ-01～Ⅳ-03、Ⅳ-11及Ⅳ-02a对供试病原细菌和真菌均表现出明显的抑菌活性,其中化合物Ⅳ-02和Ⅳ-02a尤为突出,且二者活性相近,其中Ⅳ-02对蜡状芽孢杆菌Bacillus cereus(1.184 6)、枯草芽孢杆菌Bacillus subtilis(1.88)、金黄色葡萄球菌Staphylococcus aureus(1.89)和大肠杆菌Escherichia coil(1.157 4)的MIC(抑制生长的最低浓度)值分别为0.78、12.5、1.56和1.56μg/mL,对番茄灰霉病菌Botrytis cinerea的有效抑制中浓度(EC50)为7.02μg/mL。
Isopropenyl benzimidazolone (Ⅲ) was prepared from o-phenylenediamine and ethyl acetoacetate, followed by N-acylation to give 13 benzimidazolone derivatives (Ⅳ-01 ~ Ⅳ -13) and de-isopropenyl IV-02a from IV-02, of which 9 are novel compounds which have not been reported in the literature. Its structure was characterized by 1H-NMR and GC, MS and elemental analysis. The results of antibacterial activity test showed that the compounds Ⅳ-01-Ⅳ-03, Ⅳ-11 and Ⅳ-02a showed obvious antibacterial activity against pathogenic bacteria and fungi, among which compounds Ⅳ-02 and Ⅳ-02a were prominent , And their activities were similar. Among them, Ⅳ-02 had no significant effect on Bacillus cereus (1.184 6), Bacillus subtilis (1.88), Staphylococcus aureus (1.89) and Escherichia coil (1.157 4) (MICs) of 0.78, 12.5, 1.56 and 1.56 μg / mL for MIC and 7.02 μg / mL for Botrytis cinerea, respectively.