| Wampee (Clausena lansium) is a kind of common folk medicinal plants. Modern pharmacological studies have shown that it have hepatoprotive, antiatheroscloresis, spasmolysis, nootropic, anti-HIV, immunomodulation, antiviral, antimalarial, acesodyne, cytotoxicity and antioxidation. Additionally, applications of Wampee in agricultural production have attracted a number of scientific researchers in recent years. At present, the crude extracts from different part of Wampee have a contact or repellent effect on aphids, mosquito larvae, Musca domestica, Sitophilus oryzae, Meloidogyne javanica and inhibition or lethal effect on Colletotrichum gloeosporioides, Fusarium oxysporum, Fusarium oxysporum f. sp, Magnaporthe grisea, Ralstonia dolaanacearum. Many paper showed that the effective compound of extracts is Lansiumamide B (LB).In this paper, a total of 14 compounds were synthesized by using LB as the lead compound, and their biological activity of 14 strains of fungi and a bacterium were tested. The results were as follows:1) 1 styrene group was replaced by 2-(4’-carbonyl-r-methoxy-2’,5’-diviny) ethyl,11 N-substitution introduced alkyl, alkenyl or alkynyl were synthesized and 2 saturated enamide.2) Fungal:Prolonging or shortening of carbon chain of N-substitution did not make its inhibition stronger than LB, and increasing steric hindrance of substitution did not enhance its antibacterial ability. However, methyl or ethyl on the amide nitrogen was necessary for keeping the activities, otherwise decreased. In addition, enamide group had significant impact on biological activity.3) Bacterial:The extension of N-substituted carbon chain, the hydrophobicity of the compound was increased, and the effective concentration was decreased. To increase the steric hindrance of N-substitution group could not improve the antibacterial ability of Ralstonia solanacearum. Biological activity of the derivatives with a certain positive charge was improved. Wrap this all together, the antifungal or antibacterial activity is not enhanced forthe derivatives of LB. But, the methyl or ethyl on the nitrogen and enamide were a necessary structure to maintain the activity of LB and its analogues. |
