Structure Modification Of Maleic Anhydride Compounds And Their Antibacterial Activities

The natural compounds with maleic anhydride structure is a class of substances produced by microorganisms, which have been reported in most of the class of natural compounds have good biological activity, in particular antibacterial activity, particularly as represented by the tautomycin. In this thesis, maleic anhydride as starting material, chemical synthesis17kinds of compounds with the structure of maleic anhydride, and this series of compounds were preliminary antibacterial activity.This paper starting from the tautomycin fermentation broth, which proceeds by rough handling, extraction, and purification, the purified tautomycin related structural modification. The broth by acidification, centrifugation, extraction extraction; crude extract through silica gel column chromatography, preparative liquid chromatography separation and purification; by TLC and HPLC method for simultaneous detection of the tautomycin; then through chemical modification of the tautomycin obtained ammonium tautomycin and an unknown substance with the highly active.Sclerotinia sclerotiorum and Botrytis cinerea as the experimental target, maleic anhydride compounds had antibacterial activity, these compounds have been Sclerotinia sclerotiorum and Botrytis cinerea complete inhibitory concentration and half inhibitory concentration. The same time,8kinds of maleic anhydride compounds were studying the antibacterial activity with Rhizoctonia solani, cucumber damping-off fungus, Botrytis cinerea, Fusarium and Grape anthrax.The results showed that the chemical synthesis of a series of compounds containing maleic anhydride structure to Sclerotinia sclerotiorum and Botrytis cinerea have some antibacterial activity. In particular2,3-dimethyl maleic anhydride, the half-inhibition and completely inhibited of Sclerotinia sclerotiorum were10μg/mL and55μg/mL; the half-inhibition and completely inhibited of Botrytis cinerea were35μg/mL and200μg/mL.The unknown substance from tautomycin has special effects on Sclerotinia sclerotiorum (MIC=0.05μg/mL), is10times of tautomycin (MIC=0.5μg/mL),2000times of tautomycin ammonium (MIC=100μg/mL).