P-aminosalicylic acid fluoroquinolone derivative as well as intermediate, preparation method and application thereof

Abstract

The invention discloses a p-aminosalicylic acid fluoroquinolone derivative and an intermediate, a preparation method and application thereof, and belongs to the technical field of drug synthesis. Thestructural formula of the p-aminosalicylic acid fluoroquinolone derivative is shown in the specification. In-vitro activity determination results show that part of fluoroquinolone aminosalicylate derivatives (compounds for short) and intermediates have inhibition effects on mycobacterium smegmatis; the compounds and intermediates have good inhibition activity on common pathogenic bacteria as a whole; most compounds and intermediates have better antibacterial activity on pichia pastoris as a whole; part of the compounds have good inhibitory activity on citrus canker pathogens. The p-aminosalicylic acid fluoroquinolone derivative and the intermediate thereof have potential application prospects in the fields of tuberculosis resistance, bacteria resistance, fungus resistance and citrus pathogen resistance.

Description

technical field [0001] The invention relates to the technical field of drug synthesis, in particular to p-aminosalicylic acid fluoroquinolone derivatives and intermediates, preparation methods and applications thereof. Background technique [0002] Para-aminosalicylic acid (PAS), which has long been used in the treatment of tuberculosis, has also been used in the treatment of 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 of th...

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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