Synephrine derivatives and their preparation methods and applications

Abstract

The invention discloses synephrine azole derivatives, a preparation method and application thereof, and belongs to the technical field of drug synthesis. The structural formula of synephrine derivatives is as follows. The results of in vitro antifungal activity tests showed that the MIC value of most compounds against Pichia pastoris was 0.128mg / mL, and the MIC value of individual compounds was as low as 0.064mg / mL, which was close to the positive control drug fluconazole and stronger than the tested other antimicrobials. The results of the biological activity test against citrus pathogens showed that most of the compounds had inhibitory activity against G. citrus anthracnose and P. citrus brown spot, and the inhibitory activity of individual compounds was similar to that of the positive control prochloraz, and did not show drug resistance; the target compound The inhibitory activity against citrus canker was stronger than that of synephrine. These results show that synephrine derivatives have potential application prospects in the fields of antifungal and anticitrus pathogens.

Description

technical field [0001] The invention relates to the technical field of drug synthesis, in particular to syneferinazole derivatives 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 is also used...

AI Technical Summary

Problems solved by technology

Citrus pathogens have complex differentiation, high incidence, rapid spread, and wide host range, so how to prevent and control citrus diseases has always been a worldwide problem. At present, there is no way to cure them

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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