知识与财富的链接
以香紫苏醇为先导化合物合成了 24 个β-氨基醇类衍生物,并采用菌丝生长速率法测试了目标化合物对5种植物病原菌的抑菌活性。初步构效关系分析结果表明：β-氨基醇类香紫苏醇衍生物的抑菌活性会受到苯环上连接基团性质及位置的影响,大部分间位取代衍生物的抑菌活性高于对应邻位和对位衍生物;与其他衍生物相比较,氟原子取代的衍生物 对5种供试病原菌均具有良好的抑菌活性,尤其对小麦赤霉病菌的抑菌活性最好,EC50值分别为 3.79、3.35和4.66 μg/mL。
Twenty-four β-amino alcohol derivatives of sclareol were synthesized and evaluated for their in vitro antifungal activity using the mycelia growth inhibitory rate method. The structure-activity relationship indicated that the nature and position of the substituent on the phenyl ring had an effect on the activity. Generally, the result showed that the m-substituted isomers exhibited better activity than their corresponding o/p-substituted isomers. Compared with the other derivatives, compounds containing fluoro group proved to have excellent fungicidal activities against Fusarium graminearum with EC50 values of 3.79, 3.35, and 4.66 μg/mL, respectively.
