Studies On Synthesis And Biological Activities Of Osthole Derivatives

Osthole is a Nature Compound, is also named Osthol, Its chemical name is 7-methoxy-8-isopentenyl coumarin, It's extracted from some plants of Umbelliferae, such as Cnidium fruits, is a major composition of Cnidium fruits. It's structure is following:This Compound is mainly researched and applied in medicine at present,and hardly have research and application in agricultural products.But It has been some research showed that Osthole have biological activities of insecticidal and bacteriostatic.So this years more and more research institutions begin research on Osthole,especially on Osthole's structure modification, researchers want to improve osthole's biological activities by structure reformation,and get a new leading compound just like spinosad,which is a high efficiencial and low-residuce biological pesticide. This subject is also a hot issues at home and abroad.In this paper, the author has got five new osthole derivatives from osthole-crystal,which is extracted and purified from Cnidium fruits, then by reasonable structure designing, structure optimization. These five new osthole's derivatives are verified by reactions of functional groups and infared spectrum(IR), and tested by biological activity. primary tests showed that osthole's derivatives T₂'s and T₃'s antibacterial activity is better than osthole's,this two derivatives's EC₅₀ is respectively 26.48ug/mL and 20.76ug/mL, but osthole's EC₅₀ is 43.99ug/mL.In general, in these five derivatives T₂and T₃'s antibacterial activity is better than the other derivatives, and derivatives T₂ and T₃ both contain fluorine atoms(F), this is maybe the reasons of their high antibacterial activity, and It's have important guiding function to further researching osthole's structure and biological activity.