Study On The Synthesis And Antifungal Activity Of Stilbenes

Stilbenes are products of stress found in plants,having many biological activities,such as anticancer,antioxidation,reducing blood lipids,protecting cardiovascular system and antifungal activity.In recent years,there have a great deal of pharmacological research on antifungal activities.On the market,antifungal drugs are mainly polyene drugs such as amphotericin B;three azole such as fluconazole,ketoconazole,itraconazole;allylamine such as terbinafine and so on.However,antifungal agents have fungal resistance or toxic side effects.Therefore,the study of stilbenes as antifungal agents has broad application prospects.In this project,fourteen kinds of stilbenes were synthesized by two schemes.Pterostilbene is used as the basic nucleus framework.The substitution and substitution sites of benzene ring were changed while the B rings were aligned with the hydroxyl groups.Scheme one reacted with the Wittig-Horner reaction as the core,adopting hydroxyl protection,phosphorylation,Wittig-Horner reaction and deprotection acidification four steps to synthesis five stilbenes.Scheme two reacted with Heck as the core,adopting the Wittig reaction and Heck reaction to synthesis nine kinds of stilbenes.The synthesized target compounds were examined by ~1H NMR and LC-MS and determined the chemical structure.At the same time,we tested the antifungal activity of eleven kinds of stilbenes(PS-4-PS-14)in this project.The results of biological activity showed that:the target compounds PS-6,PS-9,PS-10,PS-12,PS-13 of Candida albicans SC-5314,Candida albicans 17#,Candida albicans G5 showed good activity and compared with amphotericin B showed no better antifungal activity.But the stilbenes synthesis provides a the new direction for the study of antifungal agents.It is possible to provide a low toxicity and specific antifungal drugs for the treatment of fungal infections.