P-aminosalicylic acid dihydroartemisinin derivative as well as preparation method and application thereof

Abstract

The invention discloses a p-aminosalicylic acid dihydroartemisinin derivative as well as a preparation method and application thereof, and belongs to the technical field of drug synthesis. The structural formula of the p-aminosalicylic acid dihydroartemisinin derivative is shown in the specification. An in-vitro antibacterial activity determination result shows that the overall antibacterial activity of the target compound is relatively good; an in-vitro antifungal activity determination result shows that the target compound has good antibacterial activity on pichia pastoris as a whole; citruspathogen resistance activity determination results show that the compound has inhibitory activity on colletotrichum gloeosporioides, citrus brown blotch bacteria and citrus canker pathogens; the anti-mycobacterium smegmatis activity determination result shows that the inhibition activity of the intermediates IM1'and IM2 'is very good. Therefore, it is proved that the p-aminosalicylic acid dihydroartemisinin derivative and the intermediate thereof have potential application prospects in the fields of bacterium resistance, fungus resistance, citrus pathogen resistance and tuberculosis resistance.

Description

technical field [0001] The invention relates to the technical field of drug synthesis, in particular to p-aminosalicylic acid dihydroartemisinin derivatives and their preparation methods and applications. Background technique [0002] Para-aminosalicylic acid (PAS for short) is the first discovered small molecule drug for the treatment of tuberculosis, and it is also used to treat inflammatory bowel disease. PAS amino derivatives can be divided into three categories. The first category is PAS Schiff base derivatives. The results of the study show that the synthesized target compound has lower inhibitory concentrations to Mycobacterium smegmatis and Mycobacterium bovis than PAS; 37 The inhibitory activity of Rv was stronger than that of PZA (MICs were 3.13 and 6 μg / mL, respectively). The second category is PAS hydrazone derivatives. Isoniazid (INH) and PAS were reacted to prepare compounds containing hydrazone groups. The experimental results showed that the average ratio ...

AI Technical Summary

Problems solved by technology

The citrus canker fungus has complex differentiation, high incidence, rapid spread, and wide host range. Therefore, the prevention and treatment of citrus disease has always been a worldwide problem. At present, there is no method to cure it.

During production, Bordeaux mixture and other mixed liquids containing metal copper ions are often used for sterilization, which needs to be sprayed in large quantities many times, which may not only accelerate the development of drug resistance, but also cause toxicity to soil and other probiotics

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