桧木醇衍生物的合成及抑菌活性

Synthesis and antifungal activity of hinokitiol derivatives

摘要: 桧木醇是具有䓬酚酮骨架的单萜类天然化合物, 设计并合成了17个新型桧木醇衍生物, 其结构经核磁共振波谱及高分辨质谱分析确证。抑菌活性测定结果表明，目标化合物在50 μg/mL下对水稻纹枯病菌Rhizoctonia solani、番茄灰霉病菌Botrytis cinerea、油菜菌核病菌Sclerotinia sclerotiorum、苹果树腐烂病菌Valsa mali和黄瓜炭疽病菌Colletotrichum orbiculare均表现出较好的抑菌活性，其中化合物 3a 对水稻纹枯病菌、 3j 对番茄灰霉病菌、 3m 对油菜菌核病菌的EC₅₀值分别为1.84、2.47和1.05 μg/mL，表现出比桧木醇 (2.00、11.3和5.40 μg/mL) 更优的活性。

Abstract: Seventeen novel derivatives of hinokitiol, a monoterpene with a troponoide skeleton, were designed and synthesized. Their structures were confirmed by NMR and HRMS. The in vitro bioassay results showed that the target compounds displayed satisfactory antifungal activities against Rhizoctonia solani, Botrytis cinerea, Sclerotinia sclerotiorum, Valsa mali and Colletotrichum orbiculare at 50 μg/mL. Notably, compound 3a showed favorable activity against R. solani (EC₅₀ = 1.84 μg/mL), 3j exhibited satisfied activity against B. cinerea (EC₅₀ = 2.47 μg/mL), and 3m exerted excellent activity against S. sclerotiorum (EC₅₀ = 1.05 μg/mL), which are better than hinokitiol (2.00, 11.3 and 5.40 μg/mL).