Synephrine fluoroquinolone derivatives as well as preparation method and application thereof

Abstract

The invention discloses synephrine fluoroquinolone derivatives as well as a preparation method and application thereof, and belongs to the technical field of drug synthesis. The structural formula ofthe synephrine fluoroquinolone derivative is shown in the specification. In-vitro antibacterial activity test results show that most molecules show high inhibitory activity, and the optimal inhibitoryactivity reaches 0.2 mu g / mL; in-vitro antifungal activity test results show that most of the compounds have antifungal activity, and the optimal antifungal activity reaches 0.064 mg / mL; an in-vitroanti-mycobacterium smegmatis test result shows that the target compound has the capability of inhibiting mycobacterium smegmatis, optimally 0.097 mu g / mL, which is stronger than that of all positive control drugs; the inhibitory activity of the target compound on citrus germs is higher than that of synephrine. Therefore, that the synephrine fluoroquinolone derivative has potential application prospects in antibacterial drugs, antifungal drugs, antitubercular drugs and citrus pathogen resistant drugs is proved.

Description

technical field [0001] The invention relates to the technical field of drug synthesis, in particular to synephrine fluoroquinolone derivatives and their preparation methods and applications. Background technique [0002] Synephrine is an alkaloid present in citrus plants of the Rutaceae family. Its structure is similar to adrenaline and ephedrine and has similar biological activities. Synephrine is mainly manifested as an adrenaline α receptor stimulant, and also has a certain excitatory effect on the heart β receptor, which can promote vasoconstriction, increase cardiac output, increase blood pressure, expand bronchi and trachea; can promote metabolism, burn Fat, which has a weight loss effect. In Chinese medicine, synephrine is mainly used to treat bronchial asthma and hypotension, collapse, shock, orthostatic hypotension, as well as to treat food accumulation, phlegm, gastroptosis and other diseases; synephrine injection is also used for rescue Synephrine has also achie...

AI Technical Summary

Problems solved by technology

The strains of citrus canker have complex differentiation, high incidence, rapid spread, and wide host range, so how to prevent and control citrus canker has always been a worldwide problem. At present, there is no way 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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