伪绵马酚及其衍生物的合成与体外抗真菌作用  

Synthesis and in vitro antifungal effects of pseudoaspidinol and derivatives

作　　者：林鹏飞 杨世豪 祁燕 叶连宝 唐春萍 沈志滨 

机构地区：[1]广东药科大学中药学院,广东广州510006 [2]广东药科大学药学院,广东广州510006

出　　处：《中国药物化学杂志》2018年第1期15-19,共5页Chinese Journal of Medicinal Chemistry

基　　金：广东省应用型科技研发专项(2015B020234009)

摘　　要：目的设计合成伪绵马酚及其衍生物,并考察其抑菌活性。方法基于拼合原理,通过还原、傅-克酰基化等反应合成伪绵马酚及其衍生物并鉴定目标化合物的结构;采用M38-A2微量稀释法测定绵马酚、伪绵马酚及中间体对红色毛癣菌、须癣毛癣菌及犬小孢子菌的抑菌活性。结果与结论合成了伪绵马酚、4个中间体及2个伪绵马酚衍生物;活性研究表明,伪绵马酚对犬小孢子菌、须癣毛癣菌、红色毛癣菌3种皮肤癣菌的抗菌作用最强,其MIC值分别为10、20、28.28 mg·L^(-1)。结论合成的目标化合物对3种受试真菌均具有不同程度的抑制作用,可以为间苯三酚类化合物的成药研究提供理论基础。In this work, we aimed at the synthesis of pseudoaspidinol, an isomer of aspidinol, study of the phloroglucinol derivatives for antifungal activity against Trichophyton rubrum, Trichophyton mentagrophytes and Microsporum canis. Peudoaspidinol and intermediates were synthesized by antithetical reduction reaction,Friedel-Crafts acylation. According to the United States CLSI standards for the development of M38-A2, the effects of seven compounds to Trichophyton rubrum, Trichophyton mentagrophytes and Microsporum canis were studied using microdilution method. Pseudoaspidinol, four intermediates and two pseudoaspidinol derivatives were synthesized and had the antifungal activity; meanwhile, pseudoaspidinol showed the strongest antibacterial effect and its MIC is 10 mg·L^-1 ,20 mg·L^-1 ,28. 28 mg·L^-1 ,respectively. The synthesized compounds showed different inhibition on three fungi and the present work could provide the theory to synthesize phloroglucinols.

关 键 词：伪绵马酚 拼合原理 真菌 最低抑菌浓度 间苯三酚衍生物 

分 类 号：R914[医药卫生—药物化学]