| Sclerotinia scerotiorum and Botrytis cinerea have a significant impact on the agriculture. Traditional fungicides have well controlled these diseases in the last decades. However, an increasing number of pathogens are resistant to them. In such circumstance, new fungicides are urgently needed. This paper reviewed29kinds of natural compounds with maleic anhydride unit. Most of them possessed high biological activities, which is involved in the maleic anhydride construction unit. So, this paper designed and synthesized a series of maleic anhydride derivatives. Then, their antifungal and antibacterial activities were investigated to screen compounds with high antimicrobial activity. In addition, the structure-activity relationships discussed in this paper might be helpful for the further research.Some functional groups, such as phenyl, hydroxy, carboxyl and so on, was introduced to maleic anhydride.15kinds of maleic anhydride derivatives were synthesized and characterized. Fungicide screen assays in lab were performed by detecting the mycelium growth rate. The results showed that most of the functional groups would not enhance the activity obviously. The dialkylsubstituted maleic anhydride gained high activity and2-hexane-3-methylmaleic anhydride was the best one. The MIC of S. scerotiorum was5μg/mL and the MIC of B. cinerea was2μg/mL. Their activities could not catch up with that of2,6-dichloro-4-nitroaniline. So, further research was still needed.Moreover, the MICs to another8kinds of fungus and3kinds of bacterium was detected through cylinder-plate method. The result showed that maleic anhydride derivatives owned high activities against microorganism except Mucor and Rhizopus. Among them, the dialkylsubstituted maleic anhydride had wide antifungal spectrum and dimethylmaleic anhydride was the best one. As for the antibacterial activities, the compounds with halogen could also inhibit the bacterial well. So, maleic anhydride derivatives are high value of developing utilization. |
PDF Full Text Request