12 results about "Hydroxyquinoline derivatives" patented technology

This divisional application discloses the use of a 2,8-bis(trifluoromethyl)-4-hydroxyquinoline derivative in the control or treatment of agricultural pathogenic bacteria. The structural formula of the 2,8-bis(trifluoromethyl)-4-hydroxyquinoline derivative is as follows: Bioactivity tests show that this derivative exhibits excellent inhibitory activity against two plant bacteria: rice bacterial blight pathogen and citrus canker pathogen. Compound Q-29 shows an MIC90 value of 1.56 μg / mL against both rice bacterial blight pathogen and citrus canker pathogen, significantly outperforming the control drugs thiabendazole and thiabendazole copper. The compounds involved in this invention are easy to prepare, use inexpensive and readily available raw materials, and are expected to be developed into a novel agricultural antibacterial agent.

The invention discloses a hydrogen peroxide fluorescent probe based on a 7-hydroxyquinoline derivative as well as a preparation method and application of the hydrogen peroxide fluorescent probe. The fluorescent probe and a structural formula of the fluorescent probe are shown in the specification. According to the invention, 7-hydroxyquinoline is used as a bridge, (3, 5, 5-trimethylcyclohex-2-alkenyl) malononitrile and benzothiazole-2-acetonitrile are respectively used as strong electron withdrawing groups of a fluorescent probe molecule, and pinacol phenylboronic acid ester is used as a recognition group of H2O2 and is also used as a power supply group of the fluorescent probe molecule. The fluorescent probe molecules QCN and QSN have an obvious ICT effect, so that the probe molecules QCN and QSN emit fluorescence, and the prepared fluorescent probe shows high sensitivity and high selectivity on H2O2 in a solution. The preparation method of the fluorescent probes QCN and QSN has the advantages of simple steps, easily available raw materials, solid products, easy storage, wide application prospects, and large-scale production and application.

Provided are a 7-cyano-8-hydroxyquinoline derivative, a preparation method therefor and a medical use thereof specifically, disclosed are a compound represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing same, and a use thereof in the treatment of infectious diseases or cancer. The compound has excellent antibacterial, antiviral and antitumor activity, and can be developed as a drug for the treatment of infectious diseases or tumors. The definitions of groups in the general formula (I) are the same as in the description.

The invention discloses a phenanthroline calcium complex as well as a preparation method and application thereof. According to the invention, an 8-hydroxyquinoline derivative is used as a main ligand, 5-chloro-1, 10-phenanthroline is used as an active ligand, and the main ligand and the active ligand react with Ca (NO3) 2.4 H2O to synthesize the phenanthroline calcium complex. Experimental results show that compared with human ovarian cancer cells SK-OV-3, the phenanthroline calcium complex has a very good inhibition effect on SK-OV-3 / DDP cancer cells, has small toxicity on normal HL-7702 cells, can inhibit the growth of the SK-OV-3 / DDP cancer cells in a targeted manner, shows excellent anti-tumor activity, has potential medicinal value, and can be applied to preparation of drugs for treating ovarian cancer cells, such as ovarian cancer cells, ovarian cancer cells, ovarian cancer cells, ovarian cancer cells, ovarian cancer cells, ovarian cancer cells, ovarian cancer cells, ovarian cancer cells and ovarian cancer cells. The compound is expected to be used for preparing various anti-tumor drugs.

7- or 8-hydroxy-isoquinoline and 7- or 8-hydroxy-quinoline derivatives as alpha-1-antitrypsin modulators for treating alpha-1-antitrypsin deficiency (AATD).

Provided are a 7-cyano-8-hydroxyquinoline derivative, a preparation method therefor and a medical use thereof. Specifically, disclosed are a compound represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing same, and a use thereof in the treatment of infectious diseases or cancer. The compound has excellent antibacterial, antiviral and antitumor activity, and can be developed as a drug for the treatment of infectious diseases or tumors. The definitions of groups in the general formula (I) are the same as in the description.

The present invention relates to the use of an 8-hydroxyquinoline derivative represented by general formula (I), a pharmaceutically acceptable salt thereof, a crystalline form thereof, a solvate thereof, an isotopic derivative thereof, or a prodrug thereof, in the preparation of an antiviral drug, in particular, the use thereof in the preparation of an anti-human papillomavirus drug. The definitions of each group in general formula (I) are the same as in the specification. JPEG2025537866000239.jpg24170

The application discloses application of any one of 2,8-bis(trifluoromethyl)-4-hydroxy quinoline derivatives Q-1 to Q-39 in prevention and treatment of agricultural bacterial diseases. Through biological activity tests, the derivatives show excellent inhibitory activity on two kinds of plant bacteria, i.e. rice bacterial leaf blight pathogen and citrus canker pathogen, wherein the MIC values of compound Q-29 on the rice bacterial leaf blight pathogen and the citrus canker pathogen both reach 1.56 μg / mL, and the activity is obviously better than that of thiazolyl salicylhydrazide and thiodiazole copper. 90 The compound involved in the application is low in preparation difficulty, and raw materials are cheap and easy to obtain, so the compound is expected to be developed into a new agricultural antibacterial agent.

The invention discloses an aza-binaphthol compound and a preparation method thereof.According to the aza-binaphthol compound and the preparation method thereof, Cu-TMEDA is used as a catalyst, oxygen is used as an oxidizing agent, the aza-binaphthol compound can be constructed in one step in the air atmosphere, self-coupling of 7-hydroxyquinoline derivatives can be achieved, and the aza-binaphthol compound can be synthesized in one step; the cross-coupling reaction of the 7-hydroxyquinoline derivative and the naphthol derivative can also be realized, a simple, efficient and rapid synthesis strategy is developed, and a synthesis basis is provided for the subsequent development and application of the aza-binaphthol structure compound.

The invention discloses an 8-hydroxyquinoline derivative zinc complex as well as a synthesis method and application thereof. According to the preparation method, 8-hydroxyquinoline derivatives are taken as active ligands, phenanthroline, 4, 4 '-dimethyl-2, 2'-dipyridyl or 2-(1H-pyrazol-3-yl) pyridine is taken as auxiliary ligands, the active ligands and the auxiliary ligands react with metal salt Zn (NO3) 2, and three kinds of 8-hydroxyquinoline derivative zinc complexes are synthesized. The 8-hydroxyquinoline derivative zinc complex has a good anti-cancer effect on human skin melanoma SK-MEL-5 cells, and has small toxicity on normal HL-7702 cells, so that the 8-hydroxyquinoline derivative zinc complex provided by the invention has in-vivo and in-vitro skin melanoma resisting activity, has potential medicinal value, and can be used for preparing the anti-cancer drug. The compound is expected to be used for preparing various anti-tumor drugs.

The application relates to the technical field of organic synthesis, in particular to a synthesis method of 3-hydroxyquinoline derivatives, wherein a reactant 1,2,3,4-tetrahydroquinoline compound, a catalyst and a solvent are added into a reactor, and then the reaction is carried out under the conditions of stirring and heating; after the reaction is completed, the target product 3-hydroxyquinoline derivative is obtained through post-treatment. The new synthesis method of 3-hydroxyquinoline derivatives provided by the application uses a hybrid material synthesized by coordination of Mn-containing hydrotalcite and an organic acid as a catalyst, can synthesize 3-hydroxyquinoline derivatives under mild conditions, and has the advantages of low price of raw materials, short reaction flow and mild reaction conditions.

The invention discloses an 8-hydroxyquinoline binuclear calcium complex as well as a preparation method and application thereof. According to the invention, an 8-hydroxyquinoline derivative is used as a main ligand, 4, 7-diphenyl-1, 10-phenanthroline and 1, 10-phenanthroline are used as auxiliary ligands, and the main ligand and the auxiliary ligands react with Ca (NO3) 2.4 H2O to synthesize the 8-hydroxyquinoline binuclear calcium complex. Compared with human ovarian SK-OV-3 cancer cells, the 8-hydroxyquinoline binuclear calcium complex has a good anti-cancer effect on the SK-OV-3 / DDP cancer cells and almost has no toxicity on normal HL-7702 cells, it is indicated that the 8-hydroxyquinoline binuclear calcium complex can inhibit proliferation of the SK-OV-3 / DDP cancer cells in a targeted mode, shows excellent anti-tumor activity and has potential medicinal value, and the 8-hydroxyquinoline binuclear calcium complex has good application prospects. The compound is expected to be used for preparing various anti-tumor drugs.