6 results about "Tiamulin" patented technology

The present invention provides e / zz'-pleuromutilin triazole derivatives and e / zz'-tiamulin triazole derivatives with antibacterial activity.

The application discloses application of tegaserod maleate in preparation of an antibacterial drug synergist, and proves that the tegaserod maleate can produce a synergistic antibacterial effect with a plurality of commonly used antibacterial drugs (including tylosin, tetracycline, enrofloxacin, ampicillin and the like), can significantly enhance the antibacterial activity of the antibacterial drugs on gram-negative bacteria, and reduce the drug resistance of bacteria to the antibacterial drugs; the antibacterial composition composed of the tegaserod maleate and the antibacterial drugs can be used for preparing a drug for treating escherichia coli infection, and the synergistic antibacterial mechanism is mainly to destroy the inner and outer membrane permeability of bacteria, regulate the proton motive force of bacteria, inhibit the activity of bacterial efflux pumps, interfere with the energy metabolism homeostasis of bacteria and induce the bacteria to produce oxidative stress. The application provides a new technical strategy for the treatment of clinical escherichia coli infection, and has important clinical application value and industrialization potential.

The application discloses a teramycin ketoprofen injection and a preparation method thereof, and belongs to the field of veterinary injections, and is characterized by the following formula components: teramycin, ketoprofen, a catalytic factor, an antioxidant and an injection solvent; the catalytic factor is a polyamide amine dendrimer; and the antioxidant is a mixture of one or more than two of thio-glycerol, sodium metabisulfite or sodium bisulfite. The application has the beneficial effects that the teramycin and the ketoprofen are used in combination, no pH regulator is needed after the polyamide amine dendrimer is added, and an aqueous injection is obtained by the combination of the two, has a rapid effect, is rapidly absorbed after administration, has a short action time, can play a synergistic role in sterilization and inflammation, can not only increase the curative effect of a single drug, but also improve the drug stability and the bioavailability.

The invention particularly relates to a production method of a tiamulin key intermediate N, N-diethylaminoethanethiol in the technical field of medicines, and the production method comprises the following steps: reacting vinyl chloride with thiourea hydrochloride to generate an intermediate isothiourea salt, reacting the isothiourea salt with diethylamine, and finally carrying out alkaline hydrolysis to prepare the N, N-diethylaminoethanethiol. The preparation method disclosed by the invention is high in product yield, good in purity, low in production cost, green and pollution-free by taking water as a solvent, the two-step reaction is carried out in one pot, the intermediate isothiourea salt does not need to be separated, the production period is shortened, and the preparation method is suitable for industrial production.

The invention discloses a pleuromutilin compound as well as a preparation method and application thereof, and belongs to the technical field of medicine synthesis. The compound is a polysubstituted aryl amide thioether pleuromutilin derivative, and is synthesized by the following method: pleuromutilin is taken as a raw material, methylsulfonylation is performed on a C-22 side chain terminal hydroxyl group, a nucleophilic substitution reaction is performed on the pleuromutilin and a sulfydryl-containing aromatic intermediate, and nitryl is reduced to obtain a target compound. According to the pleuromutilin compound provided by the invention, key groups of a parent nucleus are reserved and optimized, the binding capacity and physicochemical properties of the compound and an action target are enhanced by introducing a thioether bond and a polysubstituted aryl amide group, and an in-vitro antibacterial activity test shows that the pleuromutilin compound has strong inhibitory activity on various pathogenic bacteria and can be used for preparing antibacterial agents. The activity of part of the compounds is superior to that of clinically common medicines tiamulin and valnemulin. The compound is suitable for preparing medicines for preventing and / or treating bacterial infectious diseases, and is used for developing novel and efficient antibacterial medicines.

This invention relates to the field of medicinal chemistry, and more particularly to the application of truncated pleurotin derivatives in the preparation of therapeutic drugs for drug-resistant Mycoplasma gallisepticum infections. Through screening the obtained truncated pleurotin derivatives, this invention yielded compounds with significant inhibitory activity against tiamulin-resistant Mycoplasma gallisepticum. Oral administration experiments showed a cure rate of up to 70%, significantly superior to the same dose of tiamulin, demonstrating effective resistance overcoming and significant therapeutic efficacy. These truncated pleurotin derivatives, as novel veterinary drug formulations for the prevention and treatment of chronic respiratory diseases in chickens caused by Mycoplasma gallisepticum infection, provide an effective solution to the problem of Mycoplasma gallisepticum resistance.