Synthesis And Application Of 3 - Substituted Indole Derivatives

Indole as one of the most important heterocyclic compounds, has been considered to be possessing certain biological activities, such as anticancer, anti-tumor, lowering blood pressure, anti-inflammatory effects, antiemetic effects and so on. In recent years, indole compounds are becoming increasingly significant in drug research and development. A considerable amount of effort has been made to find indoles with various biological activities and select certain agents for leads in drug discovery research. On account of their potent biological activities, indoles have continued to attract the interest of chemists and biologists alike in drug discovery.In order to find novel, high anti-cancer activity of small molecule drugs, according to the literatures published in recent five years, we use the principle of active structure stitching, marine natural products indole alkaloids meridianins was chosen as the lead compound, introduce the five-member ring, pyrazole in the 3 position of indole, and then get amides, imines and the reduct products of the imine, which are in total of 34 compounds in three kinds.The structures of all the compounds were confirmed by IR, 1H NMR, 13 C NMR, ESI-MS and take compound D01 for structural analysis as an example.To explore the more widely use of the synthesed compounds, xanthomonas oryzae is used for growth inhibition test. The preliminary bioassay results showed that: compound C01 is the most promising compounds, which can inhibit the growth of bacterial either in 100 μg/mL or in 200 μg/mL and the rate of inhibition is(80 ± 7.6)% and(83 ± 4.1)% respectively,which is better than Bismerthiazol.While compound D07 and D09 are similar to Bismerthiazol.