17 results about "Echinocandin" patented technology

The present invention relates to an echinocandin compound, and a preparation method therefor and the use thereof. Specifically, disclosed in the present invention are an echinocandin B deoxidation analogue and a biosynthesis method therefor. The echinocandin B deoxidation analogue has a good antifungal activity.

This invention discloses a primer-probe combination for detecting Candida auris and its drug-resistant mutation sites. The Candida auris drug-resistant mutation sites include azole resistance mutation sites: mutation sites A395T and A428G in the ERG11 gene, and an anti-echinocandin resistance mutation site: mutation site C1916T in the FKS1 gene. The primer-probe combination includes primer and probe sequences as shown in SEQ ID NO. 1-13, and corresponding kits and detection methods are also provided. In this invention, the primer-probe combination is prepared as a lyophilized reagent, eliminating the need for detection system preparation and directly detecting the nucleic acid extracted from the sample. It features simple operation, good stability, and wide applicability. Furthermore, by detecting the sample, it is possible to quickly determine whether the sample is positive for Candida auris and whether Candida auris drug-resistant mutations have occurred, while also identifying the drug-resistant mutation targets, meeting clinical needs and achieving precision medicine.

The present disclosure provides a pharmaceutical composition comprising an echinocandin analog and a preparation method for the pharmaceutical composition. Specifically, the present disclosure provides a pharmaceutical composition, comprising a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, a solubilizer, and a buffer. The composition has excellent stability.

The invention discloses a class of euphorbia kanane type triterpenoids as well as a preparation method and application thereof. The euphorbia kanane type triterpenoids are extracted and separated from Chinese quassia tree, four of the euphorbia kanane type triterpenoids are new compounds, and the rest of the euphorbia kanane type triterpenoids are known compounds. The applicant finds that most of the compounds show remarkable anti-neuroinflammation activity through activity screening. In an MPTP-induced PD mouse in-vivo model, part of the compounds can significantly improve the impaired movement behavior of PD mice; in addition, MPTP-induced brain tissue inflammatory response can be effectively inhibited, and a protection effect on dopaminergic neurons is achieved.

The application provides a echinocandin drug impurity, a preparation and purification method thereof and application. The echinocandin drug impurity has a structure shown in formula I: the echinocandin drug impurity is obtained by reacting micafungin sodium and a protonic acid aqueous solution, and high-purity echinocandin drug impurity is obtained after chromatographic purification. The echinocandin drug impurity obtained by the application can be used for quality control of echinocandin drugs as a control sample for establishing an analysis method.

The invention discloses an application of celecoxib or a pharmaceutical salt thereof in preparation of an antifungal drug synergist. An antifungal drug is selected from an azole antifungal drug, an allylamine antifungal drug or an echinocandin antifungal drug. The azole antifungal drug is selected from the group consisting of fluconazole, voriconazole, itraconazole, posaconazole and isavuconazole; the allylamine antifungal drug is selected from terbinafine; the echinocandin antifungal drug is selected from caspofungin. In-vivo and in-vitro experiments prove that when the celecoxib is combined with the azole antifungal drug and the allylamine antifungal drug terbinafine, a synergistic antifungal effect is shown, and when the celecoxib is combined with the echinocandin antifungal drug caspofungin, an additive effect is shown. Celecoxib and fluconazole are combined for use, so that the survival rate of fungal infected animals can be increased, and toxicity to wax moth larvae and mammalian cells is low.

Compositions and methods for controlling plant pathogens and / or for increasing plant yield and health are provided. Compositions comprise at least one antifungal compound or derivative or variant thereof from the lipophilic cyclic hexapeptide echinocandin family active against and can control at least one or more pathogens that cause plant disease and an agriculturally acceptable adjuvant. Compositions may also comprise boron containing echinocandins that are useful for the treatment or control of plant pathogens. Compositions may comprise additional antifungal agents. The compositions may be used as inoculants for plants to control plant disease. Therefore, methods for controlling plant disease and increasing yield by applying an effective amount of the composition to a plant, plant part, or area of cultivation of plants are provided.

The present invention relates to echinocandin cyclic peptides and to processes for preparing echinocandin cyclic peptides.

The present invention relates to an echinocandin analogue and a preparation method therefor. The compound can be used for preventing or treating fungal infection, or for preventing, stabilizing or inhibiting fungal growth or killing fungi. An exemplary compound is represented by formula I, wherein the definitions of R1, R2, R3 and G groups are as described in the description.

To provide echinocandin analogs for use in the prevention or treatment of fungal infections, or for use in preventing, stabilizing, or inhibiting fungal growth or killing fungi.SOLUTION: Provided is a compound represented by formula I or a pharmaceutically acceptable salt thereof, or an isomer thereof.SELECTED DRAWING: None

Provided are a novel echinocandin drug impurity compound, a preparation method therefor, and the use thereof. Compared with the structure of drug micafungin, the echinocandin drug impurity compound has one more hydrophobic acyl side chain. The method comprises first dissolving a side chain active ester in a solvent, adding a basic catalyst, and then adding an appropriate amount of a FR179642 compound for reaction. The provided high-purity echinocandin drug impurity can be applied to quality control of the echinocandin drug as a reference standard for establishing analysis methods.

The subject disclosure relates to a method of synthesizing aerolite analogs using an aerolite variant containing aspartic acid (ASP7) or glutamic acid (GLU7) at position 7, replacing the previously characterized asparagine at position 7. Selective semi-synthetic analogs produced using the ASP7 and GLU7 variants exhibit improved antifungal activity as compared to the ASN7 aerotoxin variant. The ASP7 and GLU7 variants of aerotoxin and compositions thereof are useful for the treatment of fungal and parasitic infections as well as cancer.

The present disclosure provides a pharmaceutical composition comprising an echinocandin analog and a preparation method for the pharmaceutical composition. Specifically, the present disclosure provides a pharmaceutical composition, comprising a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, a solubilizer, and a buffer. The composition has excellent stability.

The invention discloses a self-assembled nano synergistic antibacterial system constructed on the basis of Surfactin and application of the self-assembled nano synergistic antibacterial system in prevention and control of filamentous fungi. According to the preparation method, the excellent amphipathy of Surfactin is utilized, the emulsifying effect and the bactericidal synergistic effect of Surfactin are exerted at the same time, hydrophobic antibacterial active ingredients are self-assembled and wrapped to form stable nano-particles with the particle size being 20-200 nm and the PDI being smaller than or equal to 0.3 in the mass ratio of 1: 5 to 2: 1, and the FIC is smaller than or equal to 0.5 and the strong synergism is achieved. The system has the characteristic of dual purposes by one dose: Surfactin not only assists the hydrophobic antibacterial active component to penetrate through the fungal cell wall, but also cooperates with the hydrophobic antibacterial active component to trigger significant outbreak (5.8 times at most) of the active oxygen level in fungal cells, and cooperatively induces programmed death of the fungal cells. The hydrophobic active ingredients comprise plant essential oil (such as cinnamyl aldehyde), microbial source antibiotics (such as echinocandin) and broad-spectrum hydrophobic chemical bactericides (such as triazole and methoxy acrylate). The nano synergistic antibacterial system is simple in preparation process, full in biological source and free of chemical residues, the unexpected technical effects that the dosage of active ingredients is reduced by 70% or above, and the field control effect reaches up to 85% are achieved, the limitation of the known technology is remarkably overcome, and the nano synergistic antibacterial system has wide application prospects in the fields of green agriculture and food safety.

The present invention relates to an echinocandin analogue and a preparation method therefor. The compound can be used for preventing or treating fungal infection, or for preventing, stabilizing or inhibiting fungal growth or killing fungi. An exemplary compound is represented by formula I, wherein the definitions of R1, R2, R3 and G groups are as described in the description.

The invention discloses an application of epothilone and rifampicin in preparation of a synergistic anti-tuberculosis drug, and belongs to the technical field of anti-tuberculosis drugs. The core of the application is that the epothilone and the rifampicin are combined for use, and through the synergistic effect of the epothilone and the rifampicin, the bactericidal activity of the rifampicin is remarkably enhanced, the minimum inhibitory concentration of the rifampicin is reduced, and development of drug resistance of mycobacterium tuberculosis is effectively inhibited. The invention also provides a pharmaceutical preparation and a medicine box containing the two active components. According to the combined application scheme, the clinical dosage of rifampicin can be reduced, so that adverse reactions such as hepatotoxicity of the rifampicin are reduced, and the compound is suitable for treating sensitive and rifampicin-resistant tuberculosis and has important clinical value and application prospects.