Chemical Modification Of Fusaric Acid Compounds And Bioactivity Tests Of Its Derivatives

Looking for natural medicines from the plant has long been a hotspot in the field of pharmaceutical chemistry,but plant growth cycle is long,low content of active ingredients.It brings the research and development the production of natural medicine.Therefore,from more productive on organic small molecule compounds germplasm resources and looking for new structure of highly active metabolites of endophytic fungi has become an important research field in the field of natural products.Screening process and the structure of compounds,drug chemistry provides an important resource for us.Fusaric acid is produced by fusarium oxysporum strain to be toxic secondary metabolites.In the clinical applications with high value,but less research in the field of pesticides and veterinary medicine.The purpose of this paper is to systematic research fusaric acid derivatives bioactive structure-activity relationship,and achieve good active drugs.This experiment is mainly with fusaric acid as raw material,modifying the structure and measuring the pure compounds bioactivity.Study the structure-activity relationship of biological activity.The main results of the research are as follows:（1）A total of 34 compounds,including 19 fusaric acid esters derivatives,9 Amides derivatives,1 fusaric acid methyl ester analogues,2 Pyridine formic acid esters derivatives,3 the butyl benzoic acid esters derivatives.All structure compounds are confirmed.by 1H NMR,13 C NMR and MS.（2）Adopt 12 orifice plate filter paper method.Glyphosate as the positive control.Take all the compounds into lettuce seeds allelopathic activity.It is concluded that the activity of ester compounds is better than amide class,which under the 50 PPM concentration,compound HL-6,HL-33,HL-34,HL-35,HL-44,HL-45,HL-48,HL-49 respectively of root and stem of lettuce seed inhibitory activity is 100%.（3）IC₅0 of（2）activity in good compounds worthy of determination.Compound HL-33 of root of lettuce seed IC₅0 concentration is 3.63 ppm,stem 3.74 ppm.The inhibition effect is best,better than the positive control.