Synephrine fluoroquinolone derivatives and preparation method and application thereof

Abstract

The invention discloses a synephrine fluoroquinolone derivative, a preparation method and application thereof, and belongs to the technical field of drug synthesis. The structural formula of synephrine fluoroquinolone derivatives is as follows. The results of the in vitro antibacterial activity test showed that most of the molecules exhibited high inhibitory activity, with the optimum reaching 0.2 μg / mL; the in vitro antifungal activity test results showed that most of the compounds had antifungal activity, with the optimum reaching 0.064 mg / mL; The results of the in vitro anti-Mycobacterium smegmatis test showed that the target compound had the ability to inhibit Mycobacterium smegmatis, with an optimal value of 0.097 μg / mL, which was stronger than all the positive control drugs; the inhibitory activity of the target compound against citrus pathogens was stronger than Synephrine. Thus, it is proved that synephrine fluoroquinolone derivatives have potential application prospects in antibacterial drugs, antifungal drugs, antituberculosis drugs and anti citrus pathogen drugs.

Description

technical field [0001] The invention relates to the technical field of drug synthesis, in particular to a synephrine fluoroquinolone derivative and a preparation method and application thereof. Background technique [0002] Synephrine is an alkaloid present in citrus plants of Rutaceae, its structure is similar to epinephrine and ephedrine and has similar biological activity. Synephrine is mainly manifested as adrenergic alpha receptor stimulant, and also has a certain excitatory effect on cardiac beta receptors, which can promote vasoconstriction, increase cardiac output, increase blood pressure, dilate bronchi and trachea; can promote metabolism, combustion fat, which has the effect of losing weight. In traditional Chinese medicine, synephrine is mainly used for the treatment of bronchial asthma and hypotension, collapse, shock, orthostatic hypotension, and the treatment of food accumulation, phlegm and sputum removal, gastroptosis and other diseases; synephrine injection...

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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