Synthesis And Antifungal Activities Of 4-hydroxycoumarin Derivatives

Coumarin compounds and their derivatives occur widely in the natural products with a range of biological activities,and coumarin-containing compounds widely used in the fields of pharmaceuticals,agrichemicals and dyes.As its colorful biological activity,its contribution to medicine is gradually deepened.In the view of development of new pesticides historical,from the present in plants,animals and microbial secondary metabolites is an effective way to find lead compound.Given that most natural products have low activity,the stability of weak drug-like defects,the need for targeted structural modifications to the development of pesticide molecules is important.This paper aims to use natural product 4-hydroxycoumarin as a lead molecule,by structure modification,synthesisize and antibacterial activity to screen low toxicity,no residual pesticides.We used 4-hydroxycoumarin derivatives and ?-keto ester to synthesize 19 kinds and 16 kinds pyrone ring furan ring and coumarin derivatives,in which 15 kinds of coumarin and pyrone and 14 furan ring and coumarin haven't been reported.Target compounds were confirmed by 1HNMR,13C NMR,IR,EI-HRMS and some of the compounds by X-Ray.From the preliminary analysis of data at concentration of 50?g/mL against Botrytis cinerea,Colletotrichum copsica,Alternaria solani,Gibberellazeaeand Rhizoctorziasolani six common agricultural diseased pathogen,the biodata shows,some compounds have excellent biological activity,EC50 data showed that compounds I-6c and I-7b have significant inhibitory activity against Botrytis cinerea(0.08-0.09 ?MOl/mL);Compound ?-6c showed good inhibitory activity against Colletotrichum copsica,inhibitory concentration(EC50 values 0.04 ?mol/mL).