Fluoroquinolone derivatives of p-aminosalicylic acid and their intermediates, preparation methods and applications

Abstract

The invention discloses a fluoroquinolone derivative of p-aminosalicylic acid, an intermediate, a preparation method and an application thereof, and belongs to the technical field of drug synthesis; the structural formula of the fluoroquinolone derivative of p-aminosalicylic acid is as follows; in vitro antibacterial activity assay The results showed that the antibacterial activity of the target compounds against bacteria was generally good; most of the compounds had good antibacterial activities against Pichia pastoris, and some compounds were even more active than the positive control drugs; The inhibitory activity of mycobacteria is stronger than that of most positive control drugs; some target compounds have inhibitory activity against citrus pathogens; the fluoroquinolone derivatives and intermediates of p-aminosalicylic acid of the present invention have antibacterial, antifungal, antituberculous and antibacterial properties. The field of citrus pathogens has potential application prospects.

Description

technical field [0001] The invention relates to the technical field of drug synthesis, in particular to fluoroquinolone derivatives of p-aminosalicylic acid and intermediates thereof, a preparation method and applications thereof. Background technique [0002] Para-aminosalicylic acid (PAS) is an antibacterial drug used to treat tuberculosis. It is also used to treat inflammatory bowel disease by inhibiting NF-κB and scavenging free radicals. Mainly used to treat tuberculosis. [0003] PAS amino derivatives can be divided into three categories. The first class is the PAS Schiff base derivatives. The research results show that the synthesized target compounds have lower inhibitory concentrations against Mycobacterium smegmatis and Mycobacterium bovis than PAS; pyrazinamide (PZA) and the Schiff base derivatives of PAS, against H 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 d...

AI Technical Summary

Problems solved by technology

Its damage to citrus leaves, branches and fruits will form a typical canker spot symptom. If it is not treated in time, the disease will spread very quickly, which will seriously endanger the production of citrus and affect economic benefits.

Citrus pathogenic fungi have complex differentiation, high incidence, rapid spread, and wide host range, so how to prevent and treat citrus canker has always been a worldwide problem. At present, there is no way to cure it

In production, mixed liquids containing metal copper ions such as Bordeaux mixture are commonly used for antibacterial, 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. Therefore, a new type of anti-citrus bacteria is developed. drug imminent

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