474 results about "Antifungal drug" patented technology

The invention aims at providing chemical synthesis and preparation of an aromatic heterocyclic pyridine and the analogs thereof to obtain derivatives and analogs of a plurality of series of aromatic heterocyclic pyridine and medicinal salts or salts having the following formulas or prodrugs, and the preparation, a pharmacologically activity experimental method and pharmacologically activity thereof are provided. The definitions of dotted line, ring A, ring B, X1, X2, X3, X4, R1, R2 and R3 in formula I are shown in the description. The invention provides the aromatic heterocyclic pyridine derivatives and analogue with antibacterial and antifungal activities, also provides the application thereof as antibacterial and antifungal drugs and the application thereof in concomitant use with other known antibacterial and antifungal drugs and with drugs for curing bacteria infection coupled with various complicating diseases such as inflammation, virus, immune system diseases and the like, and also provides the preparation method of the aromatic heterocyclic pyridine analogs.

A method for simultaneously treating mucositis and fungal infection in a mammal in need thereof, said method comprising administering to said mammal an effective amount of an anti-mucositis and anti-fungal pharmaceutical composition consisting of a tetracycline compound in an amount that is effective to simultaneously treat mucositis and fungal infection, but has substantially no antibiotic activity.

An alkyl substituted triazazole type antifungal compound for preparing the antifungal medicines, and its various enantiomers, diaisomers, Nox and precursors are disclosed.

The invention belongs to the organic chemical field and relates to a method for preparing a medical compound chlorphenesin; wherein, the chlorphenesin belongs to an antifungal drug. For more than ten years, the product is internationally applied in necessities, such as medical soaps, soaps, ointments, nail polishes, etc. The product is also an intermediate product for preparing chlorphenesin carbamate. The invention has the advantages of easy preparation method and technique operation, easy industrialized production, high safety and stable product quality.

The invention relates to a quick diagnostic kit used for testing four or more than four kinds of invasive candidas and an application method thereof. The quick diagnostic kit is characterized in that the kit is internally provided with fluorescent quantitative PCR reaction liquid containing specific primers and fluorescent probes corresponding to the candidas which are at least four kinds as well as positive control materials and negative control materials of the candidas which are at least four kinds; Ct value tested by a fluorescent quantitative PCR tester is used for judging. The kit has the characteristics of good specificity and high sensitivity; due to double control of high specificity amplification of the primers and high specificity hybridization of the fluorescent probes, the false positive is low; therefore, the invention can be used for simultaneously testing four kinds of invasive candidas which have different sensitivities for clinical first-line antifungal drugs such as fluconazole and the like in a simple, convenient, rapid, special and sensitive way.

An improved antifungal composition for topical application to the skin and nails comprises: (1) an allylamine antifungal compound; (2) an aliphatic alcohol substituted with an aromatic substituent in which the allylamine antifungal compound is soluble to a degree that a therapeutically effective concentration of the allylamine antifungal compound can be applied topically in solution; (3) a lower aliphatic alcohol in which the aromatic alcohol is soluble; and (d) water or a water-compatible solvent mixture. The allylamine antifungal compound can be terbinafine or naftifine. The aliphatic alcohol substituted with an aromatic substituent can be benzyl alcohol or phenethyl alcohol. The lower aliphatic alcohol can be ethyl alcohol or isopropyl alcohol. In an alternative, the composition can further comprise an additional antifungal compound. Another aspect of the invention is a method for treatment of a fungal infection of skin or nails comprising administering the antifungal composition of the present invention topically to the skin or nails in an amount therapeutically effective to treat the fungal infection.

The invention relates to an extracellular antibacterial lipopeptide of plant endophytic Bacillus subtilis Jaasedl and a separation and purification method. The distribution range of the molecular weight of the extracellular antibacterial lipopeptide is mainly between 1,000Da and 2,200Da. The extracellular antibacterial lipopeptide contains an Iturin homologue, a Fengycin homologue and a Surfactin-like Compound homologue. The extracellular antibacterial lipopeptide is a group of uncommon antibacterial lipopeptide mixture produced by a single bacterial strain. The separation and purification method of the extracellular antibacterial lipopeptide comprises the following steps of: after salting out to obtain the crude extract of the antibacterial lipopeptide by using ammonium sulfate from the fermentation liquor of the endophytic Bacillus subtilis Jaasedl, performing Sephedex G-25 molecular sieve chromatography, Cellulose DEAE-52 anion exchange chromatography and FPLC300SB-C18 column chromatography successively, wherein 34 to 37 min of collecting peak has bacteriostatic activity; detecting by Tricine-SDS-PAGE after concentrating; and achieving electrophoretically pure at only one strip to obtain pure extracellular antibacterial lipopeptide. The antibacterial lipopeptide has extremely high research and application value for the development of broad-spectrum antifungal medicaments, and has wide application prospect for natural quality protection of crops and pesticide residue reduction.

The invention discloses a multifunctional microemlusion gel preparation and a preparation process thereof, and belongs to the technical field of medicines. The preparation mainly comprises bulk pharmaceutical chemicals (such as non-steroidal anti-inflammatory drugs-diclofenac sodium, ibuprofen, indometacin, antifungal drugs-ornidazole, antiviral drugs-ganciclovir, hormone drugs-dexamethasone, local anesthesia drugs-lidocaine and irritants-menthol), a cationic polymer and a microemlusion, can further comprise gel or a thickener, and can be used for transdermal drug delivery and local drug delivery. The preparation process is simple, convenient, good in stability and pollution-free. Compared with existing cream and gel, the preparation has the advantages that a novel action mechanism is adopted, the accumulative penetration amount of unit area of drugs is remarkably increased, a certain slow-release effect is achieved, and the drug delivery frequency and the drug delivery amount can be reduced; a chemical penetration enhancer and a conventional preservative are not added, a certain bacterial inhibition effect is achieved, the skin irritation is avoided, and the use safety of the drugs is improved.

The invention relates to a submicroemulsion antifungal drug spray preparation. The preparation mainly comprises the following components: an antifungal chemical synthetic drug, lecithin serving as an emulsifier, a transdermal absorption penetration enhancer and a skin protectant, soybean oil or other essential oils serving as an oil soluble diluent, glycerin serving as an isoosmotic adjusting agent, oleic acid serving as a co-emulsifier and a transdermal absorption penetration enhancer, azone serving as a transdermal absorption penetration enhancer, vitamin E serving as an antioxidant and a skin protectant, ethyl alcohol serving as a transdermal absorption penetration enhancer, natural essential oil serving as a transdermal absorption penetration enhancer, an antibacterial natural drug and essence. The submicroemulsion antifungal drug spray preparation has the advantages that the solubility and the uniformity of oil soluble antifungal drugs in water are increased, the transdermal absorption of the drugs is enhanced, the drugs are fed into dermis, and the absorption and utilization ratios of the drugs are increased, so that the effects of the antifungal drugs are increased; in the meantime, a cosolvent with side effects is avoided from being used, so that toxic and side effects caused by drugs entering whole body blood circulation systems and the stimulation to the skin are reduced, and the efficacies of protecting the skin and improving the looks are provided.

The invention relates to a preparation method of effective fractions of shining wintersweet leaf, a preparation method and a use of a preparation thereof, in particular to an application of the effective fractions of the shining wintersweet leaf and the preparation thereof in drugs used for preventing and treating respiratory system diseases as well as in anti-cold drugs, antimicrobial drugs, anti-inflammation drugs, antiviral drugs, antifungal drugs, etc. In the invention, the volatile effective fractions and non-volatile effective fractions are added to the crude drug of the shining wintersweet medicinal material with a weight ratio of the actual extraction amount of the shining wintersweet to the effective fractions being 1.0-2.6:0.5-3.5, thus the effective fractions of the shining wintersweet leaf are obtained. A preparation of the effective fractions of the shining wintersweet can be made into granules, soft capsules, capsules, drop pills, tablets, compound capsules, dispersible tablets, etc. In the invention, the preparation of the shining wintersweet is deeply developed, which ensures that the preparation is rich in active ingredients, has definite effective ingredients, obvious pharmacological action and significant improvement of drug action. Besides, the preparation has stable performance and controllable quality, is safe and reliable, has less dosage, and is favorable for transportation and storage of the medicine as well as for patients to take.

The present invention relates to medicine technology, and is 3-substituted piperazine triazonyl alcohol as new antifungal compound and its salt. The substituting radical may be in any position of heterocycle, and the compound may be single or multiple substituted. The said compound may form salt with several kinds of organic and inorganic acid. The present invention exhibits very powerful antifungal activity and may be used in preparing antifungal medicine.

The invention discloses a purification method of echinocandins antifungal drug anidulafungi. The method comprises the following steps of: (1) preparing a dry sample: adding organic solvent in a crude product of the anidulafungin to dissolve the crude product, adding silica gel after the crude product of the anidulafungin is adequately dissolved, and uniformly mixing and drying the mixture to obtain the anidulafungin dry sample; (2) pressurizing and eluting: uniformly filling the anidulafungin dry samples in the top end of a chromatographic column with silica gel, pressurizing and eluting the chromatographic column with the anidulafungin dry samples by adding elution solvent, utilizing a high-effective liquid phase chromatography to monitor, and collecting the elution solution with the anidulafungin content being greater than 98 percent; and (3) concentrating: concentrating the elution solution with the anidulafungin content being greater than 98 percent until dryness to obtain a pure product with the anidulafungin content being greater than 98 percent. By adopting the column chromatography, simplicity in operation is realized, and the equipment cost is low; the organic solvent with low toxicity and low boiling point is adopted as the elution solution, so that the subsequent recycling treatment is simple, and the environmental pressure can be greatly reduced; and the purification separation time is short, the purification effect is good, the purification yield is high, and the purification method is applicable to industrialized mass production.

The invention pertains to the technical field of medicaments, more particularly relates to a (sulfur) urea derivative with substituted semicarbazone thiochromanones and provides a novel and efficient antifungal agent. The structural formula of the derivative is shown as the Formula I. The invention also relates to a chemically acceptable compound of the derivative and a medicament combination taking the compound as an active ingredient. As a novel antifungal agent, the compound has relatively strong effect of killing pathomycete commonly seen clinically and is expected to overcome the defects that azoles antifungal medicaments widely used in clinical treatment has serious toxic side effect and is easy to generate medicament resistance, and the like. The compound is prepared by the condensation of substitutable thiochromanones and substitutable semicarbazone (sulfur) in an organic solvent.

The present invention provides a novel dominant selectable marker system in yeast that is based on an aminoglycoside, nourseothricin (NST). This compound possesses a powerful antifungal activity against Candida albicans and S. cerevisiae. The invention provides a cognate drug resistance marker for use in gene transformation and disruption experimentation in Candida albicans and Saccharomyces cerevisiae. In particular, the invention presents: 1) direct utility for gene manipulations in both clinically and experimentally relevant strains regardless of genotype and without affecting growth rate, or hyphal formation; and 2) applicability to antifungal drug discovery, including target validation and various forms of drug screening assays.

The invention relates to the technical field of medicaments, in particular to novel application of kaempferol as a synergist of anti-fungal medicaments. The anti-fungal medicaments are azole-type or polyene-type anti-fungal medicaments and based on the effective concentration of the anti-fungal medicaments, the adding ratio of the kaempferol is 0.5 to 16 mu g / ml. Tests show that when the kaempferol and the anti-fungal medicaments such as fluconazole, ketoconazole, miconazole and amphotericin B are used together, not only the anti-fungal effect is guaranteed on the premise of lowering the consumption of the anti-fungal medicaments, but also the anti-fungal medicaments can restore the function of killing the drug-resistant fungi, so that the kaempferol can be used as a synergist of the anti-fungal medicaments. The kaempferol used as the synergist of the anti-fungal medicaments can lower the consumption of the azole-type or polyene-type anti-fungal medicaments so as to reduce the toxic and side effects of the medicaments; and the kaempferol can make the anti-fungal medicaments restore the function of killing the drug-resistant fungi, so that the kaempferol can effectively treat mycotic infection, particularly drug-resistant t mycotic infection, and has quite important clinical application values.

The invention relates to a novel broad-spectrum antifungal medicine compound, a broad-spectrum antifungal medicine composition, an application of the compound or the composition in the preparation of a broad-spectrum antifungal medicine, and an application of the compound or the composition in the preparation of a medicine used for treating severe invasive infection (comprising Candida krusei) caused by invasive aspergillosis and / or Fluconazole-resistant Monilia and / or severe infection caused by Scedosporium and fusarium. The novel broad-spectrum antifungal medicine compound and the broad-spectrum antifungal medicine composition have extensive and strong antifungal activity and better dynamic property and safety. For deep mycotic infection, the novel broad-spectrum antifungal medicine compound and the broad-spectrum antifungal medicine composition are better than the original voriconazole in the aspects of the antibiotic activity and the medicine resistance and is better than amphotericin B in the aspects of safety and effectiveness; and compared with the formerly applied voriconazole, Fluconazole, itraconazole and amphotericin B, the novel broad-spectrum antifungal medicine compound and the broad-spectrum antifungal medicine composition have reinforced medicine effect, less adverse reaction and good safety.

The invention relates to a triazole alcohol derivative and a preparation method and application thereof. The chemical structure of the triazole alcohol derivative is as shown in the formula I. The invention also provides salt of the compound, a pharmaceutical composition, a preparation method and application. The compound of the invention has strong antifungal activity, has advantages of low toxicity and wide antimicrobial spectrum, and can be used for preparation of antifungal drugs.

A method of reducing antifungal drug resistance in which Hsp inhibitors, such as Hsp90 inhibitors, are used.

The invention relates to a triazole alcohol derivative, a preparation method and application thereof. The triazole alcohol derivative is a 2-(2, 4-difluorophenyl)-3-(1-substituted-1H-1, 2, 3-triazole-4-yl)-1-(1H-1, 2, 4-triazole-1yl)-2-propanol compound. The invention also provides a salt of the compound, a pharmaceutical composition, a preparation method and application thereof. The compound provided by the invention has strong antifungal activity, and has the advantages of low toxicity, broad antibacterial spectrum and the like, and can be used for preparation of antifungal drugs.

The invention relates to carbonyl reductase, a mutant and application thereof in preparation of antifungal drug intermediates. The invention specifically discloses xylose fermentation yeast carbonyl reductase and a mutant with improved activity thereof, encoding genes and amino acid sequences, recombinant expression vectors and recombinant expression transformants containing the gene sequences, as well as application of catalyzing asymmetric reduction of prochiral carbonyl compounds by taking the xylose fermentation yeast carbonyl reductase or corresponding recombinant expression transformants as catalysts, particularly catalyzing reduction of 2-chloro-2',4'-difluoroacetophenone and 2,2',4'-trichloroacetophenone for preparing antifungal compound precursors (R)-2-chloro-1-(2',4'-difluorophenyl)ethanol and (R)-2-chloro-1-(2',4'-dichlorophenyl)ethanol. Compared with the existing other asymmetric reduction methods, the method disclosed by the invention has the advantages of high enzymatic reaction substrate concentration, mild reaction condition, environment friendliness, high yield, high optical purity of products and the like and has excellent application prospects.

The invention provides a nitrogen methyl side chain-substituted triadimenol antifungal compound and a preparation method thereof, namely a 1-(1H-1, 2, 4-triazole-1-yl)-2-(2, 4-difluoro phenyl)-3-(N-methyl side chain-substituted amino)-2-propyl alcohol compound (comprising a racemate thereof, and an R type or S type isomer), and hydrochloride, nitrate, hydrobromide and methane sulfonate and a preparation method of the compound. The compound has a strong antifungal effect on various shallow and deep fungi; and compared with the traditional antifungal medicament in clinical practice, the compound has the advantages of high efficiency, low toxicity and wide antifungal spectrum and can be used for preparing new antifungal drugs. The structural formula of the compound is shown as follows.

The invention discloses a gambogic acid cyclized analog, a preparation method and application thereof. The semi-synthesized gambogic acid cyclized analog is obtained by the extracted and purified gambogic acid through chemical synthesis and has a structural general formula I-III as the right formula, wherein substituent groups of A ring, B ring, C ring, R1, R2, R3, R4, R5, R6, R7, R7, R8, R9, R10, R11 or / and R12 contain glycosyl group, polyhydroxy, amino acid group, acyloxy group, phosphoric acid oxygen group, sulphonic acid oxygen group, alkoxyl group, aromatic oxygen group, heterocyclic oxygen group, mercapto group, substituted mercapto group, primary amine and secondary amines groups or / and substituted primary amine and secondary amines groups, and chain hydrocarbon or and cyclic group containing oxygen, sulphur, nitrogen, carbon or / and phosphor atoms, and one or combination of the substitution groups. The gambogic acid cyclized analog has anti-tumor, antivirus, antibacterial and antifungal pharmacology activities, can be used as anti-tumor, antivirus, immune, antibacterial and antifungal medicaments, and can be applied together with the known anti-tumor, antivirus, immune, antibacterial and antifungal medicaments.

The invention relates to isopimarane diterpenoid compounds separated from fermentation products of Xylariasp.YM311647 and an application thereof, belonging to the technical field of microbes. The production strain YM311647 is collected in China Center for Type Culture Collection (CCTCC) on September 19, 2012, and the collection number is CCTCC No: M2012365. Three isopimarane diterpenoid compounds A, B and C are obtained by conventional fermentation, extraction and separation of the strain YM311647. Antifungal activity tests prove that the compounds have obvious antifungal activity and potential applications in preparation of new agricultural or medical antifungal medicaments.

The invention discloses a Paliurus ramosissimus extract with antifungal activity and preparations and applications thereof. The preparation method includes the steps of extracting terpenoids, flavonoids, alkaloids, cumarins (including glycosides and monomers of terpenoids, flavonoids, alkaloids and cumarins) and polysaccharides from a whole plant or any part of Paliurus ramosissimus with solvent, collecting extractive solution, concentrating and drying to obtain Paliurus ramosissimus extract; making into tablets, granules, ointment, gel, film, liniment, lotion and spray. The Paliurus ramosissimus extract with antifungal activity and preparations disclosed by the invention are used for preparing antifungal drugs.

The invention provides an antifungal medicament solid dispersion, and in particular relates to a posaconazole solid dispersion dispersed in a polymer skeleton. The polymer skeleton comprises two polymers, a first polymer can realize uniform dispersion or molecular dispersion of posaconazole in the polymer skeleton, and a second polymer can construct a microenvironment for improving the dissolution rate of posaconazole in an aqueous environment. Further, the polymer skeleton preferably comprises Soluplus and EudragitE100 in the weight ratio of 1:1.5-4. The posaconazole solid dispersion provided by the invention has good stability, good solubility in the gastrointestinal tract, and high bioavailability.

The invention pertains to the pharmaceutical chemistry field, disclosing sesquiterpenoids extracted from chloranthus family, combination, extraction method and application to preparation of antifungal drugs thereof. The invention also discloses an extractive of chloranthus family that has antifungal activity. The structure formula of sesquiterpenoids disclosed in the invention shows as formula I. The sesquiterpenoids, the combinations thereof and the extractive of the chloranthus family of the invention have antifungal activity.

The present invention belongs to the field of medicine synthesis technology, and is especially 1- (3-indolyl)- 6, 7-methylene dioxy-1, 2, 3, 4-tetrahydro isoquinoine compounds and analogs in the general expression as shown and with substituted hydroxyl radical or acyl radical in the 2nd position, and their preparation process and medical application. Initial pharmacodynamic research of extracorporeal rice blast mold resisting experiment and extracorporeal antitumor experiment shows that these compounds has excellent activity, so that they may be developed into antifungal medicine and antitumor medicine.

The invention provides a glycopeptide antifungal compound and a pharmaceutically acceptable salt thereof, a preparation method and application thereof, and a pharmaceutical composition containing the active component. The glycopeptide antifungal compound has a general structural formula shown as below; n equals to 1, 2 or 3; and R represents monosaccharide or disaccharide, wherein the monosaccharide is glucose, galactose, xylose, rhamnose, mannose, ribose, glucosamine or acetyl glucosamine, and the disaccharide is maltose or lactose. Compared with existing clinical antifungal drugs, the compound provided by the invention has advantages of high efficiency, low toxicity and broad antibacterial spectrum, etc.; therefore, the compound can be applied to preparation of antifungal drugs. The preparation method provided by the invention successfully introduce different glycosyls onto primary amino group of Caspofungin, and has advantages of simple process and high yield.

The invention provides an antifungal drug composition for external use, and a preparation method of an external preparation, and application of the composition in treating superficial fungal infections, such as tinea manus and pedis, tinea corporis, tinea cruris, tinea unguium, tinea versicolor and oidiomycosis cutis. The drug composition contains terbinafine or pharmaceutical salt thereof, sertaconazole or pharmaceutical salt thereof, and any one or multiple pharmaceutically acceptable excipient. An experimental study shows that the terbinafine or pharmaceutical salt thereof and the sertaconazole or pharmaceutical salt thereof have obvious synergistic effect when the proportion thereof in the drug composition for treating the superficial fungal infections is (1: 10) to (5: 1)(w / w). The antifungal drug composition for treating the superficial fungal infections has the advantages of being good in security, excellent in curative effect, short in treatment course, high in curing rate, low in relapse rate and the like.

A topical treatment for skin disorders and diseases comprising a combination of at least one antifungal agent and at least one hydroxy acid agent having a pH−pKa value of 0.5 or more formulated into shampoos, creams, lotions, gels, sprays, foams, pads, films, patches, and solutions for treatment of skin disorders and diseases in both humans and animals.