2 results about "Tiamulin" patented technology

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 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.