109 results about "Rhodanine" patented technology

The invention provides compounds that inhibit PIM kinases and / or CK2, and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, vascular disorders, pathogenic infections and certain immunological disorders.

The invention discloses a liquid reagent for determining N-acetyl-beta-D-glucosaminidase, which takes 5-(4-(3-methoxyl-phenylmethene-)-rhodanine-3-qmmonium acetate-N-acetylamino-beta-D-glucoside as substrate and is prepared by adding proper buffer solution, surfactant, preservative, stabilizer and the like. The liquid reagent has the advantages of large solubility of the substrate, strong stability, high detection sensitivity, convenient clinical detection, low detection cost and small outside interference for the detection result of N-acetyl-beta-D-glucosaminidase.

The invention discloses a measuring method for cyanides in cyanide-containing wastewater of a gold mine. In order to solve the problem that a great number of foams are produced by heating and distilling under an acidic condition, a defoaming agent GC-1 is added into a cyanide-containing wastewater sample to inhibit activities of a surfactant in wastewater, so that the water sample does not produce foams in a distilling process; phosphoric acid and Na2-EDTA are added into the water sample, and heated and distilled in a medium with pH lower than 2, so that cyanide ions are separated from complex cyanide by utilizing the characteristic that the complexing capacity between the metal ions and the EDTA is higher than that between the metal ions and the cyanide ions, the cyanide ions are distilled in the form of hydrogen cyanide, and the content of the cyanide ions is titrated by silver nitrate after the cyanide ions are absorbed by a sodium hydroxide solution. Under an alkaline condition, the cyanide ions act with the silver nitrate to form soluble sliver-cyanogen complex irons (Ag(CN)2<->), and the excessive sliver ions react with 5-(4-dimethylaminobenzylidene)rhodanine indicator liquor, so that the solution is changed into orange red from yellow, thereby ending the measurement. The method has the advantages of obvious effect and accurate measured result, and is simple to operate and easy to grasp.

Disclosed herein are rhodanine derivatives, a method for the preparation thereof, and a pharmaceutical composition containing the same. The rhodanine derivatives have inhibitory activity against protein phosphatases (PPase) such as PTP1B, Prl-3, LAR, CD45, Cdc25A, Cdc25B, Cdc25C, Yop, PP1 and VHR, and can be applied for the prevention and treatment of PPase-caused diseases, including autoimmune diseases, diabetes, impaired glucose intolerance, insulin resistance, obesity, cancers, etc. when the inhibitory activity thereof is modulated.

This invention describes compounds and pharmaceutical compositions useful as inhibitors of ubiquitination. The compounds and compositions of the invention are useful as inhibitors of the biochemical pathways of organisms in which ubiquitination is involved. In particular, the compounds and compositions are useful for treating diseases caused by viruses such as poxviruses and retroviruses. The invention further provides for methods of treating smallpox, Herpes virus and HIV infection in patients using the compounds and compositions of the invention.

The invention relates to a rhodanine derivative and an application thereof. In the rhodanine derivative, a group containing a multi-ring aromatic ring group or / and a multi-ring heteroaromatic ring group is taken as an electron donor, and 2-(1',1'-dicyan)rhodanine is taken as an electron acceptor; or a group containing a multi-ring aromatic ring group or / and a multi-ring heteroaromatic ring group is taken as an electron donor, 2-(1',1'-dicyan)rhodanine is taken as an electron acceptor, and a conjugated heteroaromatic ring group is taken as a bridging group. The obtained rhodanine derivatives have unique photoelectric chemical performance, and can be taken as photosensitizers of dye-sensitized solar cells.

The invention provides B crystal form epalrestat and a preparation method thereof. The method comprises the following steps: taking rhodanine acetic acid and alpha-methylcinnamaldehyde as raw materials and reacting to generate epalrestat crude product suspension; adding a first acid solution into the epalrestat crude product suspension; then heating and melting, carrying out centrifugal treatment,washing a filter cake and drying to obtain an epalrestat crude fine product, wherein the mole ratio of an acidic substance in the first acid solution to the rhodanine acetic acid is (3 to 4.5) to 1;adding low-carbon alcohol into the epalrestat crude fine product; after heating and melting, keeping for pre-set time; then cooling to 20 to 30 DEG C; carrying out the centrifugal treatment and dryinga filter cake to obtain an epalrestat fine product. According to the B crystal form epalrestat and the preparation method thereof, provided by the invention, the yield and purity of B crystal form epalrestat products are easy to improve and the content of 2Z-isomer impurities is reduced.

A glycoprotein and / or a glycopeptide which are a test substance is heated in the presence of a pyrazolone derivative, an isoxazolone derivative, a hydantoin derivative, a rhodanine derivative, a maleimide derivative, or the like under a basic condition to cleave and label a post-translational modification group for analysis, thereby enabling analysis of a post-translational modification of a serine residue and / or a threonine residue.

The invention discloses an N-methyl ciprofloxacin (rhodanine unsaturated ketone) amide derivative and a preparation method and an application thereof. The N-methyl ciprofloxacin (rhodanine unsaturated ketone) amide derivative adopts the following chemical structural general formula I (shown in the specification); and in the formula I, Ar represents a benzene ring or a substituted benzene ring or a furan ring or a pyridine ring. The N-methyl ciprofloxacin (rhodanine unsaturated ketone) amide derivative disclosed by the invention implements superposition of three pharmacophores of a chiral tricyclic fluoroquinolone skeleton, amide and rhodanine alpha, beta-unsaturated ketone, so that the antineoplastic activity of a new compound is improved, and the toxic or side effects on normal cells are reduced, and the N-methyl ciprofloxacin (rhodanine unsaturated ketone) amide derivative can be used as an antineoplastic active substance for developing an antineoplastic medicament of a brand-new structure.

The invention discloses a rhodanine derivative and a preparation method thereof, wherein the structure of the rhodanine derivative is shown in the specification; the preparation method comprises the following steps of: mixing a first rhodanine derivative of Bc1-2 inhibitor with an anti-tumour effect, 5-p-hydroxyphenyl-1,2-benzodithiole-3-thioketone, a condensing agent and alkali in a solvent according to the mass ratio of 1:(1-2):(1-2):0.001:0.1, reacting at 25-100 DEG C for 0.5-24 hours, and purifying, thereby obtaining the rhodanine derivative, wherein X comprises one of F, Br, Cl and Ph; R comprises one of CH2Ph, CH2CH(CH3)2 and CH(CH3)2; and the invention further relates to an anti-tumour drug composed of the rhodanine derivative and pharmaceutically acceptable carriers. By means of the manner, the prepared rhodanine derivative contains pharmacodynamic groups capable of releasing gas signal molecule hydrogen sulphide, is capable of generating anti-tumour synergistic effect, and has good inhibition effect on tumour cells; furthermore, the anti-tumour activity of the rhodanine derivative disclosed by the invention is stronger than that of the first rhodanine derivative before being modified.

The invention discloses a 3,5-disubstituted rhodanine anti-apoptosis protein Bc1-2 inhibitor as well as preparation method and an application thereof. The compound has a structure of a general formula I. The compound disclosed by the invention has high inhibitory activity on Bc1-2 and can be used for preparation of medicines for preventing or treating related mammal diseases caused by abnormal expression of anti-apoptosis protein Bc1-2. The invention also relates to a pharmaceutical application of a composition of the compound with the structure of the general formula I. The structural formula is as shown in the specification.

Disclosed are novel rigidified compounds having a rhodanine-like residue and at least one aryl or heteroaryl residue linked to the rhodanine-like residue, whereby a core structure of these compounds, as defined in the specification, is characterized as having one or zero free-to-rotate bonds. Also disclosed are pharmaceutical compositions containing these rigidified compounds and uses thereof for modulating the activity of heparanase and hence in the treatment of heparanase-associated diseases and disorders, and uses thereof for modulating the activity of heparin-binding proteins and hence in the treatment of heparin-binding proteins-associated diseases and disorders as well as in the treatment of medical conditions that are at least partially treatable by rhodanine or a rhodanine analog.

The invention relates to a fused ring benzoselenadiazole non-fullerene acceptor material as well as a preparation method and application thereof. The fused ring benzoselenadiazole non-fullerene acceptor material has a structure represented by a formula 1, wherein R1 is C1-C20 alkyl; Ar is an electron-donating polycyclic aromatic hydrocarbon based on benzene or thiophene; EG is an electron withdrawing group based on rhodanine or dicyanomethylidene indan-1-one; the condensed ring benzoselenadiazole non-fullerene acceptor material comprises a condensed ring benzoselenadiazole central core and electron withdrawing end groups, the condensed ring benzoselenadiazole central core is of a nitrogen bridge trapezoidal condensed ring structure, and the electron withdrawing end groups are connected tothe two ends of the central core.

This invention describes compounds and pharmaceutical compositions useful as inhibitors of ubiquitination. The compounds and compositions of the invention are useful as inhibitors of the biochemical pathways of organisms in which ubiquitination is involved. In particular, the compounds and compositions are useful for treating diseases caused by viruses such as poxviruses and retroviruses. The invention further provides for methods of treating smallpox, Herpes virus and HIV infection in patients using the compounds and compositions of the invention.

The invention relates to preparation and application of an oligomer photovoltaic donor material which is based on a 5,6-difluorobenzothiadiazole unit and has an A'(D-A)2DA' framework. The electron donating (D) unit is thiophene, bithiophene, benzodithiophene and derivatives thereof, the electron accepting (A) unit is 5,6-difluorobenzothiadiazole and derivatives thereof, and the electron accepting(A') unit is cyano-rhodanine, cyano-indandione and derivatives thereof. The oligomer has good film-forming property, high light absorption coefficient, wide light absorption range and proper energy level. Compared with a solar cell made of an A'-D-A-D-A' type small molecular photovoltaic material, the solar cell made of the A'(D-A)2DA' type oligomer shows better photovoltaic performance, and the energy conversion efficiency of a device is improved by nearly 20%.

The invention provides an antibacterial compound containing a quinoline or pyrazole heterocycle rhodanine structure and a synthetic method thereof. The antibacterial compound containing the quinoline or pyrazole heterocycle rhodanine structure has a broad antibacterial spectrum and obvious antibacterial activity on gram-positive bacteria, and minimum inhibitory concentration is 1 microgram / ml, thus the antibacterial compound containing the quinoline or pyrazole heterocycle rhodanine structure has the potential to be prepared into an antibacterial agent. The invention provides a lead compound for developing a new antibacterial agent, the synthetic method of the antibacterial compound is simple and reasonable, and production cost is low.

The invention belongs to bis(rhodanine)merocyanine sensitizing dyes, belongs to the field of organic synthetic dyes, and especially relates to a preparation method of a bis(rhodanine)merocyanine sensitizing material by taking 2-methylbenzothiazole and a rhodanine derivative as main initial raw materials. The target product is obtained by taking low-price 2-methylbenzothiazole and rhodanine carboxylate as the raw materials and performing five-step reaction. The beneficial effects comprise that: the method is simple and easy in reaction operation, small in environmental pollution, high in product purity and relatively low in cost, and is suitable for large-scale industrial production.

The invention discloses a detection reagent for N-acetyl-beta-D-glucosaminidase with high analytical sensitivity. The reagent disclosed by the invention comprises a reagent R1 and a reagent R2; the reagent takes an artificially-synthesized product 5-(4-(3-methyl-styrene)-rhodanine-3-rhodanine-acetic acid amino-N-acetamino-beta-D-glucoside as a reaction substrate, so that the sensitivity of the reagent is improved; the reagent adopts two kinds of buffer solutions, i.e., an MES (2-(N-morpholine)ethyl sulfonic acid) buffer solution and an AMP (2-amino-2-methyl-1-propanol) buffer solution, so that the catalytic action of an NAG enzyme can be promoted while buffer capacity is guaranteed, a strongly-alkaline environment is effectively improved, and the efficiency of color development is guaranteed; ingredients are reasonably matched and used, so that the overall sensitivity, specificity and accuracy of the reagent are relatively high, and the further popularized use in market is facilitated.

The invention relates to an application of 5-(4-hydroxyl-3-methoxybenzylidene)rhodanine to preparation of a medicament for treating a Parkinson's disease.

The invention relates to an organic dye, in particular to a D-N=N-pi-A organic dye, wherein D refers to an electron repulsive structure unit, N=N refers to an azo structure unit, pi refers to a coumarin conjugate structure unit, and A refers to a rhodanine electron acceptor structure unit. The invention aims to find a functional organic dye which has the advantages of high molecular tailoring properties, wide spectral response range, low synthesis cost and capacity of absorbing most visible light and can be applied to the fields such as acid dyes, fluorescent dyes, organic electroluminescent materials and dye-sensitized nano TiO2 solar cells.

The invention discloses a tertiary leucine derived chiral amine compound as well as a preparation method and application thereof. The chiral amine compound contains a tert-butyl group, a primary amine, a secondary amine or a tertiary amine functional group and has the structural formula as shown in the specification; and chiral amine and salts thereof are prepared through simple preparation steps by taking common tert-leucine as the raw material to form the chiral amine compound. The chiral amine and the salts thereof can be used for the asymmetrical Michael additive reaction between alpha, beta-unsaturated ketone and a nucleophilic reagent such as nitrocarbol, malonic ester, substituted oxazolone and the like and the asymmetrical cascade reaction between the alpha, beta-unsaturated ketone and fifth-position unsaturated rhodanine, between fifth-position unsaturated hydantoin and the alpha, beta-unsaturated ketone; and the tertiary leucine derived chiral amine compound has very high catalytic activity and stereoselectivity as well as the highest diastereoselectivity of 30 / 1 and the highest enantioselectivity of 99%, and is wide in oligomer range.

The invention discloses a levofloxacin (rhodanine unsaturated ketone) amide derivative and a preparation method and an application thereof. The levofloxacin (rhodanine unsaturated ketone) amide derivative adopts the following chemical structural general formula I (shown in the specification); and in the formula I, Ar represents a benzene ring or a substituted benzene ring or a furan ring or a pyridine ring. On the basis of a medicine molecule construction strategy of pharmacophore splice, the levofloxacin (rhodanine unsaturated ketone) amide derivative disclosed by the invention implements superposition of four pharmacophores of a chiral tricyclic fluoroquinolone skeleton, amide, rhodanine and alpha, beta-unsaturated ketone, so that the antineoplastic activity of a new compound is improved, the toxic or side effects on normal cells are reduced, and the levofloxacin (rhodanine unsaturated ketone) amide derivative can be used as an antineoplastic active substance for developing an antineoplastic medicament of a brand-new structure.

The invention provides an organic photoelectric conversion material, which has a ternary structure formed by using an indacenodithiophene derivative, benzothiadiazole and rhodanine as a base unit, wherein the structural formula is defined in the specification, R is a group selected from the following materials defined in the specification, and R1, R2, R3 and R4 are respectively and independently selected from hydrogen, fluorine, C1-C12 alkyl and alkoxy. According to the present invention, the material has good amorphous property and good solubility, and can be processed by solutions; by increasing the pi-pi conjugation length of the donor unit, the pi-electrons can be easily distributed along the whole polymer skeleton, have strong absorption in the visible and near-infrared regions, and has good energy level matching with commonly used donor polymers; and the material has excellent carrier transmission performance, and can be used in organic field effect transistors, organic solar cells and organic semiconductor devices.

The invention relates to an AIE fluorescence probe molecule, and p-nitroaniline and fluoride ion detection methods thereof in order to solve the technical problems of poor identification ability and serious fluorescence quenching of fluorescence probes in the prior art. 5-pyrenylmethylenerhodanine is prepared from pyrenecarboxaldehyde and rhodanine by a simple synthesis technology with pyridine asa catalyst. The molecule has a good aggregation-induced luminescence effect, and is a highly-sensitive fluorescence probe molecule for detecting p-nitroaniline and fluoride ions.

The invention discloses a detection reagent for N-acetyl-beta-D-glucosidase. The detection reagent comprises a reagent R1 and a reagent R2, wherein the reagent R1 comprises 10-100mmol / L of citric acidbuffer solution, 0.1-0.3g / L of substrate, 1KU / L-5KU / L of ascorbic acid oxidase, 0.01-0.03g / L of magnesium chloride, 1-10g / L of stabilizer, and 2g / L-5g / L of preservative, the reagent R2 comprises 10-100mmol / L of sodium carbonate buffer solution, 3mL / L-5mL / L of triton X-100, and 2g / L-5g / L of preservative, the citric acid buffer solution is at 25 DEG C and the pH thereof is 4-5, the substrate is 5-[4-(3-methoxy-benzophene-rhodanine)-3-ammonium acetate-N-acetylamino-beta-D-glucoside, the stabilizer is one of EDTA, EDTA-2Na, glycol, and diglycolamidic acid, and the preservative is one of NaN3, methylparaben, and 4-chloro-3,5-dimethylphenol. A synthesized substrate 5-(4-(3-methyl-styrene)-rhodane-3-acetic acid amino-N-acetamino-beta-D-glucoside is used as a reaction substrate, the substrate isrelatively low-cost, and a reactant has high color development performance, so that the reagent is more sensitive.

The invention discloses poly-rhodanine coated inorganic packing as well as a preparation method and application thereof. The preparation method comprises the following steps: dispersing inorganic nano packing in water in a suspension manner so as to obtain 0.1-25wt% aqueous dispersion; adding a rhodanine monomer into the aqueous dispersion, and stirring for 5-60 minutes at 60-95 DEG C; adding an oxidant into the aqueous dispersion to react for 0.5-6 hours at 60-95 DEG C; filtering, thereby obtaining the poly-rhodanine coated inorganic packing. An inorganic packing modification method is implemented in water phase, is free of organic solvent, and has the advantages of being simple in process, environment-friendly in procedure, high in efficiency, good in universality for various types of polar packing, and the like. In poly-rhodanine modified inorganic packing reinforced rubber, dispersion of the packing can be remarkably improved, and the interface function can be also improved.

Disclosed are novel rhodanine derivatives which are inhibitory of HIV activity. Also provided are a method for preparing the novel rhodanine derivatives, and a pharmaceutical composition for the prevention or treatment of AIDS containing the rhodanine derivatives as active ingredients. Having high inhibitory activity against HIV, the rhodanine derivatives can be effectively used in the prophylaxis or therapy of AIDS.

The invention relates to the technical field of medicines, in particular to a preparation method of epalrestat. The preparation method provided by the invention comprises the steps of mixing 3-carboxymethyl rhodanine, alpha-methylcinnamyl aldehyde, a catalyst and water, and sequentially carrying out condensation reaction and acid neutralization to obtain an epalrestat crude product, wherein the catalyst comprises a basic catalyst and a phase transfer catalyst; and mixing the epalrestat crude product with an alcohol organic solvent, and recrystallizing to obtain the epalrestat. The preparation method adopts water as a reaction solvent, and is safe and environment-friendly; the existing three procedures such as crude product preparation, acidification dissociation and recrystallization are simplified into two procedures such as crude product preparation and recrystallization, and the two procedures such as crude product preparation and acidification dissociation are combined into one, so that the procedures are simplified; and an alcohol organic solvent is adopted for recrystallization, so that recycling is facilitated.

The invention discloses a conjugated organic small molecule interface modification material, a preparation method and an organic solar cell formed by the conjugated organic small molecule interface modification material. The organic small-molecular interface modification materials SAM1, SAM2 and SAM3 are obtained through one-step condensation synthesis of p-aldehyde benzoic acid and 1,3-indanedione, rhodanine and dicyanorhodanine. According to the organic small molecule interface modification material, zinc oxide can be subjected to surface modification through physical adsorption and chemicalreaction; not only can the defect state density of hydroxyl dangling bonds on the surface of zinc oxide be reduced, but also the energy level arrangement can be optimized to reduce the electron transport barrier at the interface, thereby improving the interface charge extraction of the solar cell device and reducing the interface carrier recombination. The modification efficiency and the device efficiency of the inversion type organic solar cell prepared from the material are obviously improved. After the SAM1 is modified, the device efficiency of the PBDB-T / ITIC system is improved to 10.82%from 10.13%, and the device efficiency of the PBDB-T-SF / IT-4F system is improved to 13.25% from 12.18%.

A compound which is a thienolate of formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein R1, R3, Ring A1, n and Ring A2 are as defined herein, are found to be useful in inhibiting metallo-beta-lactamase and therefore in potentiating the activity of beta lactamase antibiotics. The compound can be used alone or in combination with a rhodanine of formula (II) or a pharmaceutically acceptable salt thereof: (II) wherein R3, Ring A1, n, Ring A2, L and Ring B are as defined herein. Treatment or prevention of bacterial infection in combination with beta-lactam antibiotic agents is also provided.