曲酸及氯曲酸衍生物的合成及抑菌活性

Synthesis and antifungal activity of kojic acid and chlorokojic acid derivatives

摘要: 以曲酸为原料，设计合成了16个曲酸衍生物（QⅠ-01~QⅠ-16）和10个氯曲酸衍生物（QⅡ-01~QⅡ-10），通过核磁共振氢谱及元素分析对其结构进行了表征。初步抑菌活性测定结果表明：所有供试化合物对苹果炭疽病菌Glomerella cingulata和番茄灰霉病菌Botrytis cinerea的菌丝生长均有不同程度的抑制作用，其中化合物 QⅠ-07 和 QⅠ-11 对苹果炭疽病菌活性最高，50 μg/mL时的抑制率分别为79.3%和86.2%；化合物 QⅡ-04 、 QⅡ-08和QⅡ-09 对番茄灰霉病菌活性最高，50 μg/mL时的抑制率分别为70.0%、70.0%和76.7%。

Abstract: Sixteen kojic acid derivatives (QⅠ-01~QⅠ-16) and ten chlorokojic acid derivatives (QⅡ-01~QⅡ-10) were synthesized from kojic acid. The structures of the synthesized derivatives were confirmed by 1H NMR and elemental analysis. Antifungal activity results indicated that all of the title compounds exhibited variable inhibitory activities against the mycelial growth of Glomerella cingulata and Botrytis cinerea. The inhibition rates of 50 μg/mL QⅠ-07 and QⅠ-11 against G.cingulata were 79.3% and 86.2%, and QⅡ-04, QⅡ-08 and QⅡ-09 against B.cinerea were 70.0%, 70.0% and 76.6%, respectively.