46 results about "Thiazole derivative" patented technology

The application belongs to the technical field of cosmetic and pharmaceutical chemistry, and discloses a 2,4-dihydroxyphenyl thiazole derivative and application thereof. The 2,4-dihydroxyphenyl thiazole derivative has the structure shown in the following formula: wherein n1 and n2 are each independently 1, 2, 3 or 4; and R is methyl or ethyl. Compared with existing peptide amido compounds, the 2,4-dihydroxyphenyl thiazole derivative of the application, while maintaining the active structure of the parent nucleus, significantly improves the solubility and physicochemical stability through molecular modification, and optimizes the pharmacokinetic characteristics. The derivative can effectively inhibit the activity of tyrosinase, and can be used as an active ingredient to prepare a novel tyrosinase inhibitor, related whitening and freckle-removing cosmetics and a drug for tyrosinase-related diseases.

A 2-aminoarylthiazole derivative or a pharmaceutically acceptable salt or solvate thereof, in particular masitinib or a pharmaceutically acceptable salt or solvate thereof, for use in the treatment of sickle cell disease in a patient in need thereof. Also, a 2-aminoarylthiazole derivative or a pharmaceutically acceptable salt or solvate thereof, in particular masitinib or a pharmaceutically acceptable salt or solvate thereof, for use in the prevention and / or treatment of acute chest syndrome (ACS) in a sickle cell disease patient in need thereof.

This invention belongs to the field of pharmaceutical synthesis technology, specifically relating to indomethacin derivatives, their synthesis methods, and applications. The derivatives possess the chemical structures described in formulas (I), (II), and (III). This invention is the first to propose a series of novel indomethacin derivatives. Furthermore, this invention also proposes a synthesis method for indomethacin derivatives, using 5-hydroxy-1-indanone as a base material, to obtain the indomethacin derivatives of this invention through a series of reactions. This synthesis method yields high-yield products that are easily separated, making it the optimal method for preparing the indomethacin derivatives of this invention. Bioassays have confirmed that the indomethacin derivatives provided by this invention exhibit good toxic activity against aphids, spider mites, and armyworms, and can be applied to the control of plant pests.

The present invention provides an aminonitrothiazole derivative for use in the preparation of a drug for preventing and treating viral infections and related diseases caused thereto, and belongs to the field of pharmaceuticals. The structure of the aminonitrothiazole derivative is shown in Formula I. Experimental results show that the compound can effectively inhibit the activity of respiratory syncytial virus, enterovirus 71, and the new coronavirus, and the inhibitory effect is better than that of the positive controls nitazoxanide and lauric acid. The compound provided by the present invention can be used to prepare a drug for preventing and / or treating viral infections, and can be used to prepare a drug for preventing and / or treating related diseases caused by viruses, and has broad application prospects.

The present invention belongs to the technical fields of medicinal chemistry and pharmacology, and discloses a thiazole derivative, its preparation method, and application. The thiazole derivative has a structure represented by formula (I) and is prepared by dissolving cedrinone and ferric acetylacetonate in a mixed solution of ethanol and ethylene glycol, adding phenylsilane, and reacting to obtain compound 2. Compound 2 is then reacted with pyridinium tribromide in THF at room temperature to obtain compound 3. Compound 3 undergoes a [3+2] cycloaddition reaction with thiourea to obtain thiazole derivative 4a. 4a is then reacted with a benzoic acid compound to obtain thiazole derivative 4. This thiazole derivative has been found to have strong tumor cell growth inhibition activity and is expected to be used as an anti-tumor drug.

The application discloses an anti-tumor matrine hydrazine thiazole derivative and a preparation method and application thereof, NaH is added into a reaction container one, then a DMF solution is added, and then aminothiourea is added into the reaction container one to stir the solution; sophoridine is added into the stirred solution to perform a reflux reaction, after the reaction is completed, a quenching reaction is performed, and then extraction, concentration drying and column chromatography separation are performed to obtain an aminothiourea matrine intermediate; the obtained aminothiourea matrine intermediate is added into a reaction container two, and an ethanol dissolving solvent is added to dissolve; the dissolved solution is added with alpha-bromo R base ethanone to perform a reaction, after the reaction is completed, concentration drying and column chromatography separation are performed to obtain the anti-tumor matrine hydrazine thiazole derivative. The anti-tumor matrine hydrazine thiazole derivative has strong anti-tumor activity, and the preparation method is simple and the reaction condition is easy to control.

The present application relates to the technical field of pharmaceutical chemistry, and particularly relates to application of nitrothiazole derivatives and hydrochloride and sulfate thereof in preparation of medicines for treating intestinal infection of poultry and livestock. The nitrothiazole derivatives synthesized by the present application have high biological activity at the cell level, and have good biological activity on bacterial enteritis of poultry and livestock, especially chicken, pig, sheep and deer, and have high application value.

The application provides a use of a nitrothiazole derivative in preparation of an antibacterial agent for inhibiting helicobacter pylori, and belongs to the field of pharmacy.The structure of the amino nitrothiazole derivative is shown as formula I.The experimental results show that the compound can effectively inhibit the growth of helicobacter pylori, and the inhibiting effect is better than that of control compounds nitazoxanide and lauric acid; the compound can effectively treat mice infected with helicobacter pylori, clear helicobacter pylori in the stomach and reduce the inflammatory response of the stomach tissue, and the treatment effect is better than that of control compounds nitazoxanide and lauric acid.The compound provided by the application can be used for preparing the antibacterial agent for inhibiting helicobacter pylori, and can be used for preparing a medicine for preventing and / or treating helicobacter pylori infection and related diseases caused by the helicobacter pylori, and has a wide application prospect.

The present invention discloses a steroidal dihydropyrazole thiazoline derivative, 3β-hydroxy-pregnane-5-en-17β-yl-5'-(substituted phenyl)-1'-(4''-phenyl-[1'',3'']-thiazol-2''-yl)-4',5'-dihydropyrazole-3'-yl. The present invention also discloses the use of the steroidal dihydropyrazole thiazoline derivative. The steroidal dihydropyrazole thiazoline derivative of the present invention has a strong inhibitory effect on nitric oxide (NO) production in RAW 264.7 mouse peritoneal macrophages induced by lipopolysaccharide (LPS), especially compound 4 in the prepared steroidal dihydropyrazole thiazoline derivative has an IC of 0.05. 50 The value is better than that of the positive control methylprednisolone, and the toxicity to cells is low. The steroidal derivative containing a dihydropyrazole thiazoline heterocycle provided by the present invention is a new structural compound, which shows higher activity than existing first-line anti-inflammatory drugs.

This provides the crystalline form of piperazinyl-thiazole derivatives. [Solution] The present invention relates to the crystalline form of 1-{(R)-2-(2-hydroxy-ethyl)-4-[2-trifluoromethyl-4-(2-trifluoromethylpyrimidine-5-yl)-thiazole-5-yl]-piperazine-1-yl}-2-(3-methyl-[1,2,4]triazole-1-yl)-ethanone, a method for producing the same, a pharmaceutical composition having the crystalline form, a pharmaceutical composition produced from the crystalline form, and the use of the same as a CXCR3 receptor modulator in the treatment of various diseases and disorders related to the CXCR3 receptor and its ligands.

The application relates to a preparation method and application of a 2-acyl benzothiazole compound, which comprises the following steps: placing sulfur ylide in a sealed tube, adding a solvent to dissolve, and obtaining a first reaction system; adding nitrosobenzene into the first reaction system, stirring at a certain temperature for a certain time, and obtaining a second reaction system; adding sodium hydrosulfide, dimethyl sulfoxide, a metal salt, potassium persulfate and an alkali into the second reaction system, heating and stirring in the sealed tube to react, and obtaining a third reaction system; and carrying out post-treatment on the third reaction system to obtain the 2-acyl benzothiazole compound.The application has the advantages that the reaction condition is mild, the price of the sodium hydrosulfide sulfur source is low, and the reaction yield is high; the substrate applicability range is wide, various substrate structures can tolerate the reaction condition, and the 2-acyl benzothiazole derivative with diversified structures can be rapidly prepared.

The application relates to methods and intermediates for synthesizing the thiazole derivative Coumpound (1) useful in treating and / or inhibiting the development or progression of diseases or disorders caused by, or associated with, herpes virus infection.

The invention belongs to the technical field of cosmetics and medicinal chemistry, and discloses a 2, 4-dihydroxy phenyl thiazole derivative and application thereof. The invention discloses a 2, 4-dihydroxy phenyl thiazole derivative, which has a structure as shown in the following formula, wherein n1 and n2 are respectively and independently 1, 2, 3 or 4; r is methyl or ethyl. Compared with the existing peptidomidogen compounds, the 2, 4-dihydroxy phenyl thiazole derivative disclosed by the invention has the advantages that the solubility and the physical and chemical stability are remarkably improved through molecular modification while the active structure of a parent nucleus is maintained, and the pharmacokinetic characteristics are optimized. The derivative can effectively inhibit the activity of tyrosinase, and can be used as an active component for preparing a novel tyrosinase inhibitor, related whitening and freckle-removing cosmetics and drugs for treating tyrosinase-related diseases.

The invention belongs to the technical field of medicinal chemistry and pharmacology, and particularly relates to a flavanone thiazole derivative as well as a preparation method and application thereof. The structural formula of the flavanone thiazole derivative is shown in the specification, and in the structural formula, R represents one of 2-iodophenyl, 2, 4-dichlorophenyl, 4-fluorophenyl, 2-bromobenzyl, 4-bromophenyl, 2-bromophenyl, 4-chlorobenzyl and 4-methylphenyl. The flavanone thiazole derivative is a flavanone thiazole ring-fused derivative, and pharmacological research shows that the compound has high liver cancer cell proliferation inhibition activity and can be applied to preparation of drugs for preventing and treating liver cancer.

The present invention discloses a benzothiazole derivative, the structure of which is shown in Formula I below. By modifying the amide group on the benzothiazole skeleton and splicing it with amino acid fragments, a series of acylhydrazone and acylhydrazide derivatives were designed and synthesized based on this structure. Tumor inhibition tests have shown that these derivatives have certain inhibitory activity against liver cancer cells and melanoma cells and can be used to prepare anti-tumor drugs, thereby providing more candidate compounds for the development of new drugs.

Provided are a crystal form of a thiazole derivative inhibitor, and a preparation method therefor and the use thereof. Particularly provided are a crystal form of a compound as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing a therapeutically effective amount of the crystal form, and the use thereof as an inhibitor in the treatment of autoimmune diseases.

An isolated pharmacologically active composition for use in the treatment of neurodegenerative diseases, the composition comprising: 0.1% to 20% (w / w) of at least one synthetic small molecule backbone selected from heteroaryl-substituted piperazine derivatives, benzothiazole derivatives or quinoline-based analogues; 50% to 95% (w / w) of at least one pharmaceutically acceptable carrier or excipient; and 0.1% to 10% (w / w) of a stabilizer, antioxidant or surfactant.

The application relates to the technical field of organic synthetic chemistry, and particularly discloses a 2-acyl benzothiazole derivative and a preparation method thereof. The method takes benzothiazole compounds and aromatic aldehyde compounds as substrates, takes polyacid such as phosphomolybdic acid as a catalyst, and generates the 2-acyl benzothiazole derivative through cross-dehydrogenative coupling in an organic solvent under the conditions of air or oxygen atmosphere and light irradiation. The application does not need a transition metal catalyst and an alkaline additive, uses oxygen as a terminal oxidant, the catalyst can be recycled and reused, the reaction condition is mild, the operation is simple, the applicable range of the substrate is wide, the chemical selectivity is high, and the product yield can reach 85%. The method overcomes the limitations of safety, selectivity and scale of the prior art, and provides an efficient, economical and environment-friendly new path for the preparation of high-value 2-acyl benzothiazole derivatives in the fields of medicine, pesticide and material science.

The present invention relates to the technical field of pharmaceutical synthesis, and specifically relates to diene thiazole derivatives and their synthesis methods and applications. The diene thiazole derivatives disclosed in the present invention are a series of brand-new compounds, which are proposed for the first time. The diene thiazole derivatives have the chemical structure shown in general formula (1). The synthesis method of the diene thiazole derivatives of the present invention uses 16-DPA as the basic raw material and obtains the diene thiazole derivatives of the present invention through a series of different reactions. The synthesis method has a high preparation yield, and the obtained product is easy to separate. It has been confirmed by biological assays that the diene thiazole derivatives exhibit good insecticidal activity against pests such as aphids, oriental armyworms, diamondback moths, and whiteflies, and can be used to prepare single-agent agricultural insecticides or mixed preparations containing the diene thiazole derivatives. #imgabs0#

Disclosed are imidazothiazole derivatives, their preparation methods, and uses. The imidazothiazole derivatives have a structure represented by formula (I): R1 and R3 are each independently selected from an optionally substituted 5- to 6-membered heterocyclic group containing 1-2 nitrogen atoms, and R2 and R4 are each independently selected from an optionally substituted aryl or heteroaryl group. The imidazothiazole derivatives have good MNK inhibitory activity, excellent selectivity, and superior in vivo hypoglycemic effects, and have broad medicinal prospects.

The present invention relates to a salt of a thiazole derivative inhibitor, a crystal form thereof, a preparation method therefor and the use thereof. In particular, the present invention relates to a salt of a compound represented by general formula (I), a crystal form thereof, a preparation method therefor, a pharmaceutical composition containing a therapeutically effective amount of the salt and / or crystal form, and the use thereof as an inhibitor in the treatment of autoimmune diseases.

This invention relates to the field of composite panels and discloses a wear-resistant and UV-resistant fiberglass-silicon core composite panel and its preparation method. The composite panel comprises melamine-faced paper, fiberglass mat, and calcium silicate board impregnated with adhesive. The adhesive includes deionized water, melamine-formaldehyde resin, modified aluminum hydroxide, organosilicon flexibility agent, and coupling agent. The modified aluminum hydroxide is prepared by reacting a functional modifier, N,N'-bis-(2,2,6,6-tetramethyl-4-piperidinyl)-1,6-hexanediamine with benzophenone derivatives and pyridylthiazole derivatives, with 3-chloropropyltriethoxysilane and grafted onto aluminum hydroxide. The organosilicon flexibility agent is prepared by modifying phenyl hydrogen-containing silicone oil with allyl polyoxyethylene ether and glycidyl methacrylate. This invention achieves an integrated structure of the panel, maintaining a surface free of blistering and cracking under complex environmental conditions, with the overall material intact and without delamination, and possessing good antibacterial, fire-resistant, and UV-resistant properties.

The application relates to methods and intermediates for synthesizing the thiazole derivative Compound 1 useful in treating and / or inhibiting the development or progression of diseases or disorders caused by, or associated with, herpes virus infection. (I)

The invention relates to a preparation method of a two-component organosilicon polyurea antifouling coating containing benzothiazole. The preparation method comprises the following steps: reacting aminopropyl double-terminated polydimethylsiloxane (APT-PDMS), polyether amine (D-400), dicyclohexylmethane-4, 4-diisocyanate (HMDI) and hexamethylene diisocyanate (HDI) to obtain organic silicon polyurea as a main chain, and then introducing a thiazole derivative 2-aminobenzothiazole (BIT) into a molecular chain of the main chain through a chemical grafting method, so as to prepare the high-temperature-resistant silicone rubber. And finally reacting to obtain the antifouling coating. The preparation method of the coating is simple, and the obtained coating has excellent mechanical properties, excellent static antifouling capacity and excellent marine service performance.

An object of the present disclosure is to provide a rubber composition from which a crosslinked rubber molded product having good softness and excellent resilience performance can be obtained. The present disclosure provides a rubber composition containing (a) a base rubber, (b) a co-crosslinking agent, (c) a crosslinking initiator, and (d) a salt of a benzothiazole derivative, wherein (d) the salt of the benzothiazole derivative includes a compound represented by the formula (1) in which a sulfur atom S2 constituting a thiocarbonyl group has a Mulliken charge of −0.190 or more.[In the formula (1), R1 to R4 are identical to or different from each other, and represent an electron-withdrawing group or a hydrogen atom, S1 and S2 represent a sulfur atom, X represents a cation component, n is an integer ranging from 1 to 4, and at least one of R1 to R4 bonding to the identical benzene ring is an electron-withdrawing group when n is 2 or more.]

A system (100) for the preparation of piperazine-linked imidazo[2,1-b]thiazole derivatives as anticancer agents, antioxidants and anti-inflammatory agents, comprising: a) a reaction chamber (102) configured to enable multiple chemical reactions for the synthesis of piperazine-linked imidazo[2,1-b]thiazole derivatives; b) a heating unit (104) operatively connected to the reaction chamber (102) and configured to provide controlled temperature conditions ranging from room temperature to reflux temperature; c) a cooling unit (106) operatively connected to the reaction chamber (102) and configured to maintain cooling temperatures during operation of the reaction chamber (102); d) a stirring unit (108) operatively connected to the reaction chamber (102) and configured to provide continuous mixing of the reaction components; e) a solvent supply system (110) configured to supply reaction solvent to the reaction chamber (102); f) a reagent supply system (112) configured to supply reaction reagents to the reaction chamber (102); g) a purification unit (114) configured to purify the synthesized piperazine-linked imidazo[2,1-b]thiazole derivatives by column chromatography; and h) a sample collection unit (116) configured to collect and store the resulting product after each reaction performed in the reaction chamber, the sample collection unit (116) being connected to a delivery system configured to return the collected sample to the reaction chamber for subsequent reactions.

The invention relates to a gallic amide bridged thiazole derivative as well as a preparation method and application thereof. The invention discloses a novel gallic acid derivative, namely a gallic amide bridged thiazole derivative, and a preparation method and application of the gallic amide bridged thiazole derivative. The gallic amide bridged thiazole derivative disclosed by the invention is a novel compound and has important significance on synthesis and discovery of anti-inflammatory drugs.

The embodiment of the invention discloses a 5-nitrothiazole derivative, a pharmaceutical composition and application. The 5-nitrothiazole derivative in the embodiment of the invention is a compound with a structure as shown in a formula I or an isomer, a prodrug, a stable isotope derivative, a hydrate, a solvate and a pharmaceutically acceptable salt thereof; the 5-nitrothiazole derivative is prepared by taking 2-bromo-5-nitrothiazole as a raw material through a nucleophilic substitution reaction, the synthesis process is simple, the yield is high, and industrial production is easy to realize; the 5-nitrothiazole derivative provided by the embodiment of the invention can effectively inhibit the growth of micro-aerobic bacteria, especially has a remarkable inhibition effect on helicobacter pylori (drug-resistant strains and / or sensitive strains), and can directly enhance the treatment effect on helicobacter pylori infection. Therefore, the 5-nitrothiazole derivative has a relatively good application prospect in preparation of antibacterial drugs.

The present application belongs to the field of medicine, and relates to a polysubstituted thiazole derivative and application thereof in disease treatment. Specifically, the present application relates to a compound of formula I or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the compound of formula I or the pharmaceutically acceptable salt thereof, and application of the compound of formula I or the pharmaceutically acceptable salt thereof in treating or preventing a dihydroorotate dehydrogenase-mediated disease, including a tumor, a viral infection and an immunological disease.