112 results about "Quinolone" patented technology

The invention belongs to the field of antibiotic analysis and detection, and discloses a quinolone drug SERS (Surface Enhanced Raman Scattering) detection method based on an improved silver nano-substrate and a spectral angle matching model. An improved Lee-Meisel method is adopted to synthesize silver nano sol with precisely controlled particle size, molecular adsorption is realized by utilizing electrostatic interaction of a positively charged quinolone drug and negatively charged silver nano particles, and a high-density Raman enhanced hot spot is formed after an agglomeration agent is added; the SERS spectrum is collected at the excitation wavelength of 785 nm and the integral time of 10 s, qualitative distinguishing of drugs is achieved by combining a spectrum angle matching model, and quantitative detection is achieved by constructing a standard curve through the linear relation between the characteristic peak intensity and the drug concentration logarithm. The detection limit of the four drugs is as low as 1.03-1.16 ppb, the classification accuracy rate reaches 100%, the method is obviously superior to existing similar methods, the detection matrix range is wide, such as animal food and dairy products, and universality and high sensitivity are both considered.

The invention provides a compound as shown in a formula (I), and a stereoisomer, a tautomer, an isotope label, nitrogen oxide, a solvate, a polymorphic substance, a metabolite, ester, pharmaceutically acceptable salt or prodrug thereof, or a pharmaceutical composition thereof, which have better antibacterial and anti-inflammatory effects, can be used as an antibiotic, and can be used for preparing a pharmaceutical preparation for preventing and treating diseases. The compound can treat infection caused by pathogenic microorganisms resistant to erythromycin and telithromycin, and simultaneously acts on double targets of ribosome and topoisomerase.

This application discloses a linker and its preparation method. The linker includes pharmacophore P, pharmacophore Q, and deoxynucleotides and / or deoxynucleotide derivatives connecting pharmacophore P and pharmacophore Q. Pharmacophore P is obtained by removing the protecting group from group B, and pharmacophore Q is obtained by removing the protecting group from group X. Group B is obtained by chemically modifying the benzylquinolone carboxylic acid pharmacophore, and group X is obtained by chemically modifying the zenomeprazole pharmacophore. The linker is prepared by linking group B and group X with deoxynucleotides and / or deoxynucleotide derivatives to form the linker, including solid-phase synthesis technology. The method of this application can automatically synthesize molecular probes or bivalent drugs containing two pharmacophores, thereby replacing the traditional stepwise linking method, enabling efficient construction of screening libraries, and allowing control of the spatial distance and spatial orientation of the pharmacophores by adjusting the number and base arrangement of deoxynucleotides.

The invention discloses a multi-emission composite nano ratiometric fluorescent probe for detecting fluoroquinolone antibiotics and a preparation method of the multi-emission composite nano ratiometric fluorescent probe. The CdTe-Tb-UMP composite nano ratiometric fluorescent probe with double ligands is prepared by taking metal terbium ions (Tb < 3 + >) as central ions and respectively taking uridine monophosphate (UMP) and CdTe quantum dots with red fluorescence emission as bridged ligands. ENR is further coordinated with Tb < 3 + >, energy is transferred to Tb < 3 + > through an antenna effect, so that characteristic green fluorescence of Tb < 3 + > is turned on, and fluorescence of CdTe quantum dots is almost kept unchanged. On the basis, a portable nursing point testing system is further constructed, and the portable nursing point testing system comprises an intelligent mobile phone detector and a wearable fingertip sensor integrated with a micro-fluidic chip and is used for on-site rapid detection of the ENR. The paper-based chip shows rapid and sensitive fluorescence response, and the detection limits of the spectrograph and the paper-based sensor on the ENR are 4.7 nM and 13.1 nM respectively. The probe can be applied to detection of ENR in actual environment water samples, food and drugs.

The invention relates to the technical field of organic chemistry, and particularly discloses an amide derivative containing a thiazole oxime structure as shown in a general formula 8 and a preparation method and application of the amide derivative. The derivative shows remarkable antibacterial activity on staphylococcus aureus, escherichia coli, pseudomonas aeruginosa and fluoroquinolone-resistant escherichia coli, particularly has a remarkable effect on gram-negative bacteria, has broad-spectrum antibacterial potential and can be used for preparing drugs for treating related bacterial infection, and the activity of part of compounds is superior to that of a control drug.

The invention discloses a passive sampling device and method for specifically enriching quinolones and tetracyclines antibiotics, and relates to water body detection. Firstly, a hydrogel thin film prepared from ZIF-C as an adsorbent is adopted as a binding film, ZIF-C particles are uniformly dispersed on the surface of the binding film, specific adsorption of quinolones and tetracyclines antibiotics can be achieved, then the binding film, a diffusion film and a polyether sulfone filtering film are sequentially stacked to be assembled into an o-DGT device, o-DGT is put into a water body, and through diffusion and adsorption, the specific adsorption of the quinolones and tetracyclines antibiotics can be achieved. The method realizes the extraction and detection of quinolone and tetracycline antibiotics by the DGT technology.

The application relates to quinolone aminothiadiazole compounds, a preparation method and medical applications thereof, and belongs to the technical field of chemical synthesis. The quinolone aminothiadiazole compounds are shown in a general formula I. The compounds have good inhibitory activity on one or more of gram-positive bacteria, gram-negative bacteria and fungi, can be used for preparing antibacterial and / or antifungal drugs, have no obvious drug resistance, and can provide more efficient and safe candidate drugs for clinical anti-infection treatment.

The present invention provides methods, compositions, and combinations for treating cancer via combined use of a compound of formula I or a pharmaceutically acceptable salt, ester, solvate and / or prodrug thereof, wherein A, Q, n, m, R7, R8, V, X1, X2, X3, X4, X5, X6, and X7 are as defined herein, and at least one therapeutically active agents selected from immunotherapeutics, anticancer agents, and anti-angiogenics.

The present invention relates to stable synergistic insecticidal composition for synergistic and effective control of various insect pests including entire sucking pests complex. The present invention also relates to a process for preparation thereof.

Provided are a quinolone analogue represented by formula (I), or a pharmaceutically acceptable salt, a stereoisomer, a racemate, a deuterated compound, or a solvent compound and a pharmaceutical composition thereof, and uses thereof in the preparation of drugs for treating tumors, autoimmune diseases, or diseases caused by bacteria, fungi or viruses.

The present application relates to a kind of metal single atom and nanoparticle composite catalyst and its preparation method.By the reasonable proportioning of metal salt, dicyanediamine and urea dosage, high loading single atom and nanoparticle composite catalyst is prepared by simple two-step pyrolysis method, the preparation method is simple, metal loading can be controlled, with good reproducibility and applicable to a variety of metal salt (such as Co, Cu, Ni, Fe, Mn, etc.).Single atom and nanoparticle composite catalyst obtained by the present application can construct a large number of active sites, significantly improve the catalytic activity and stability of catalyst, for degrading sulfonamide organic pollutants, quinolone organic pollutants and tetracycline organic pollutants, or for depolymerization lignin, all of which show excellent catalytic activity, and the degradation or depolymerization effect is higher than that of currently reported catalyst.

The invention discloses a magnetic nano-material and application thereof in extraction of fluoroquinolone compounds, and the magnetic nano-material is prepared by mixing an aqueous solution of Fe3O4 (at) SiO2 microspheres with NH2 modified surfaces and an ethanol aqueous solution of fluorinated graphene according to a volume ratio of (2-4): (1-3) and then stirring. The magnetic nano material is used as a magnetic solid-phase extraction adsorbent and can be used for extracting fluoroquinolone compounds in a sample. The magnetic nano material disclosed by the invention not only can efficiently extract various fluoroquinolone compounds in simple matrixes such as water, milk and the like, but also can directly enrich and extract various fluoroquinolone compounds in complex matrixes such as cosmetics and the like without tedious and time-consuming purification steps; and high-throughput detection of various trace fluoroquinolone compounds in a sample can be realized.

Generally, the present invention provides novel quinolone compounds and pharmaceutical composition thereof which may inhibit cell proliferation and / or induce cell apoptosis. The present invention also provides methods of preparing such compounds and compositions, and methods of making and using the same.

The present application belongs to the technical field of quorum quenching enzyme preparation, and particularly relates to a multi-target quorum quenching enzyme preparation and a preparation method and application thereof, such as being mainly used for inhibiting the virulence factors of Pseudomonas aeruginosa, and including acyl homoserine lactone acyltransferase AiiO protein and 3-hydroxy-4-oxoquinolone 2,4-dioxygenase AqdC protein, and the mass ratio of the two is 20:(1-25); such as being mainly used for inhibiting the virulence factors and the synthesis of biological membranes of Pseudomonas aeruginosa, and further including deferiprone, and the mass ratio of AiiO, AqdC and deferiprone is 20:(1-25):(0.695-2.78), the present application can target the Las, Rhl and PQS of Pseudomonas aeruginosa, the yield and stability of the prepared AqdC protein are both high, the two types of enzymes are used in combination after the regulation amount, and the virulence factors regulated by different quorum sensing pathways in Pseudomonas aeruginosa are effectively inhibited; the regulation amount of deferiprone is used in combination with the two types of quorum quenching enzymes, and the virulence and biological membranes of Pseudomonas aeruginosa can be effectively inhibited in a comprehensive manner.

The application discloses a method for simultaneously detecting 32 kinds of veterinary drug residues in fecal pollution, and belongs to the technical field of veterinary drug residue detection. The method comprises the following steps: taking a fecal pollution sample, adding Na2EDTA-Mcllvaine buffer solution and acetonitrile for extraction, centrifuging the sample after salting-out to obtain an organic phase, purifying the organic phase through an LPAS purification column, collecting the purified liquid, concentrating and blowing dry, redissolving, filtering, and obtaining a to-be-detected liquid; detecting the to-be-detected liquid by using an ultra-high performance liquid chromatography-triple quadrupole mass spectrometer, gradient elution; and quantitatively detecting 32 kinds of veterinary drugs by using a matrix matching standard curve method. The method is simple in operation and good in purification effect, can effectively remove interfering substances such as fat and protein in the fecal pollution, significantly reduces the matrix effect, is suitable for simultaneously, quickly and accurately detecting 23 kinds of sulfonamides and 9 kinds of fluoroquinolones in pig, chicken, cow and duck fecal pollution, and has good accuracy and precision.

The invention relates to quinoxaline derivatives as anti-cancer drugs. Specifically, the invention relates to azaquinolone compounds of formula (I) and their use in medicine.

The application belongs to the technical field of photocatalytic materials and the field of environmental governance, and discloses a preparation method and application of a heterojunction photocatalytic material for degrading fluoroquinolone antibiotics. The catalytic material is an S-type photocatalytic material, and the heterojunction photocatalytic material can be prepared through a simple hydrothermal method. By controlling the addition amount of NH2-MIL-68(In), Bi2MoO6 / NH2-MIL-68(In) heterojunctions with different component contents are obtained. Experimental results show that when the Bi2MoO6 / NH2-MIL-68(In) (BMN-2) photocatalytic material prepared by the application is applied to photocatalytic degradation of ofloxacin in water, 100% of the ofloxacin can be degraded after visible light irradiation for 90 minutes. In addition, the photocatalyst also has good photocatalytic degradation performance for ofloxacin in actual water. The heterojunction photocatalyst prepared by the application has good visible light response and excellent antibiotic degradation performance, and has good application prospect in the field of photocatalytic degradation of antibiotics.

The application belongs to the field of biological medicine and health, and discloses a preparation method of a novel tricyclic indole pyridone carboxylic quinolone molecule. The method is based on the fact that only one N atom is inserted into the bicyclic quinoline nucleus of the pharmacodynamic skeleton "quinoline-4-ketone-3-carboxylic acid" of fluoroquinolone drugs, and then a novel tricyclic indole pyridone carboxylic fluoroquinolone drug molecule is ingeniously constructed, a new structure antibacterial lead compound is found through in-vitro activity evaluation, and a basis is provided for the creation of a new drug with independent intellectual property rights to overcome the drug resistance and adverse reactions of existing drugs.

Provided herein are pharmaceutical compositions comprising a quinolone compound for irritable bowel syndrome, especially provided is the use of the quinolone compound, in particular 1-cyclopropyl-6-fluoro-1, 4-dihydro-8-methyl-7- (2-amino-3-cyano-5-pyridyl) -4-oxo-3-quinoline-carboxylic acid or a pharmacologically acceptable salt, a hydrate, a solvate or a deuteride thereof for preventing or treating irritable bowel syndrome of a human or an animal.

The application provides a macrolide derivative and a preparation method and application thereof, relates to the technical field of medicinal chemistry, and the macrolide derivative is a compound with a general structure shown in the following formula I: in the formula, A is selected from any one of alkynyl, alkenyl or piperazine; R is selected from any one of H or F; X is selected from any one of CH or N, Y is selected from any one of methyl, ethyl or cyclopropyl, and n is an integer in the range of 2-6. The macrolide derivative is connected by different lengths of ether hydrocarbons at the 3-position, thereby avoiding the problem that the instability of a synthesized compound is caused by using an ester group as a side chain to connect a quinolone group. The application successfully prepares a macrolide derivative with double targets, and the antibacterial activity of the macrolide derivative is obviously better than the antibacterial activity of erythromycin, telithromycin, clarithromycin and ciprofloxacin which only have single targets.

Compounds of Formula (I), (I,) wherein the substituents are as defined in claim 1. The invention further relates to herbicidal compositions which comprise a compound of Formula (I) and to the use of compounds of Formula (I) for controlling weeds, in particular in crops of useful plants.

The invention relates to quinoxaline derivatives as anti-cancer drugs. Specifically, the invention relates to azaquinolone compounds of formula (I) and their use in medicine.

The invention discloses a prawn enterohepatic cytozoon disease comprehensive prevention and treatment and green culture method, and relates to the technical field of aquaculture and disease prevention and control. The method comprises the following steps: adding the following four medicines into a prawn feed for feeding: an antiprotozoon triazine compound, wherein the addition amount of the antiprotozoon triazine compound is 0.2-0.3% of the weight of the feed; the addition amount of the fluoroquinolone antibacterial agent is 0.5%-0.8% of the weight of the feed; the adding amount of the medicine for astringing dampness and sores is 0.8%-1% of the weight of the feed; and the addition amount of the promoting coagulant is 0.1-0.2% of the weight of the feed. Through the synergistic effect of quadruple drugs, the immunity and organ repair capacity of prawns are enhanced, the treatment effect is remarkable, and the passive state that no safe and effective chemical drugs or antibiotics can kill EHP spores in prawns at present, and once the EHP spores break out, the EHP spores can only be controlled to spread and reduce loss is changed; the worldwide problem that sick prawns stop growing or grow extremely slowly and only eat but not grow is solved, and the survival rate and the growth rate of the prawns are increased.

This invention provides a method for preparing quinolone compounds, belonging to the field of pharmaceutical intermediate synthesis technology. The invention involves mixing a phenolic compound, a fluorosulfonating reagent, an organic base, and an organic solvent to perform a fluorosulfonation reaction, yielding a fluorosulfonated product. The fluorosulfonated product, a borate ester compound, a transition metal catalyst, a ligand, an inorganic base, and a solvent are then mixed and coupled to obtain the quinolone compound. The purpose of this invention is to address the problems existing in current synthetic methods for C7 carbon-carbon bond-substituted quinolone compounds, such as long reaction steps, low yields, and numerous hazardous processes. It provides a new synthetic method for quinolone compounds, requiring inexpensive and readily available chemical reagents, featuring a short process, high yield, and avoiding the use of hydrogen or diazonium salts, making it suitable for both rapid laboratory synthesis and industrial production.

The present invention relates to a compounds according to general formula (I), which acts as an inverse agonist of PqsR (the currently only known receptor for the Pseudomonas Quinolone Signal (PQS), sometimes also referred to as MvfR); to a pharmaceutical composition containing one or more of the compound(s) of the invention; to a combination preparation containing at least one compound of the invention and at least one further active pharmaceutical ingredient; and to uses of said compound(s), including the use as a medicament, e.g. the use in the treatment or prophylaxis of a bacterial infection, especially a Pseudomonas aeruginosa or Burkholderia infection.

This invention provides the application of Evodia rutaecarpa root extract in the preparation of antifungal agents, belonging to the field of agricultural fungal control technology. The active ingredient of the Evodia rutaecarpa root extract is naturally derived and easily obtained; its unique chemical structure and novel mechanism of action effectively avoid the problem of pathogen resistance caused by the concentrated mechanisms of action of existing fungicides, filling the market gap for quinolone-based plant-derived pesticides. The Evodia rutaecarpa root extract exhibits a precise antifungal spectrum and significant inhibitory effect, showing obvious inhibitory activity against soil-borne and interplant-borne plant fungi that are serious threats in agricultural production, such as Phytophthora tobaccoii, Fusarium equisetifolium, Colletotrichum gloeosporioides, and Fusarium moniliforme.

Provided are a compound of formula (IA) and other quinolone compounds, wherein variables are as defined in the description, and use of the compounds in the treatment or prevention of diseases or disorders such as autoimmune diseases, allergic diseases, inflammatory diseases, and pain.

This invention provides a simple and environmentally friendly method for synthesizing 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid ester. Unlike the conventional method of first converting excess carboxylic acid to the corresponding acyl chloride using thionyl chloride, removing the excess thionyl chloride, adding fresh solvent, and then adding the corresponding alcohol to form the ester, this method uses the following order of addition: thionyl chloride → ethylene glycol monomethyl ether → thionyl chloride → ethylene glycol monomethyl ether. The thionyl chloride and ethylene glycol monomethyl ether are added alternately. Under a certain amount of solvent, the generated ester is cleverly utilized to promote the dissolution of the acyl chloride, while simultaneously reducing the absolute content of the acyl chloride in the solution. This allows the reaction mixture to form a solution state, promoting complete conversion of the carboxylic acid and driving the reaction forward. This avoids the defect of the carboxylic acid raw material being encapsulated due to the poor solubility of the intermediate, resulting in incomplete reaction.

This invention relates to the preparation method and pharmaceutical application of cyanide-bridged quinolone imidazoles and their analogues, belonging to the field of chemical synthesis technology. The cyanide-bridged quinolone imidazoles and their analogues are shown in general formulas I-III. These compounds exhibit inhibitory activity against one or more Gram-positive bacteria, Gram-negative bacteria, and fungi, and can be used to prepare antibacterial and / or antifungal drugs. This offers the potential to provide more safe, efficient, and diverse candidate drugs for clinical antimicrobial therapy, helping to address increasingly serious clinical treatment problems such as drug resistance, persistent pathogenic microorganisms, and emerging harmful microorganisms. The raw materials used in their preparation are simple, inexpensive, and readily available, with high synthetic yields, making them significant for anti-infective applications.