61 results about "Thiazole derivative" patented technology

The invention discloses an anti-tumor matrine hydrazine thiazole derivative and a preparation method and application thereof.The preparation method comprises the steps that NaH is added into a first reaction container, then a DMF solution is added, thiosemicarbazide is added into the first reaction container, and the solution is stirred; adding sophocarpidine into the stirred solution to perform reflux reaction, performing quenching reaction after the reaction is finished, and performing extraction, concentration drying and column chromatography separation to obtain a thiosemicarbazide sophocarpidine intermediate; adding the obtained thiosemicarbazide matrine intermediate into a reaction container II, and adding a dissolving solvent ethanol for dissolving; adding alpha-bromo-R-ethyl ketone into the dissolved solution for reaction, concentrating and drying after the reaction is finished, and performing column chromatography separation to obtain the anti-tumor matrine hydrazine thiazole derivative. The anti-tumor matrine hydrazine thiazole derivative is high in anti-tumor activity, the preparation method is simple and convenient, and reaction conditions are easy to control.

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.

The present invention relates to the field of synthesis of thiazole compounds, and in particular to a 2,4,4-trimethylthiazole derivative and a synthesis method thereof. The present invention, in the presence of an alkali, uses calcium carbide, hydrogen sulfide and propargylamine compounds as main raw materials for reaction; calcium carbide is used as a solid alkyne source, acetylene gas is released by depolymerizing calcium carbide with hydrogen sulfide, and acetylene gas is reacted with propargylamine compounds, thereby synthesizing 2,4,4-trimethylthiazole derivatives. The present invention uses H2S to depolymerize calcium carbide to synthesize 2,4,4-trimethylthiazole derivatives, wherein safe, stable and easily available calcium carbide is used as a raw material, no transition metal catalysis and high-pressure resistant equipment are required, and toxic and harmful H2S gas is reasonably used. The synthesis method of the present invention has more prominent advantages in "atom economy" and "green chemistry".

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 invention discloses a benzothiazole derivative fluorescent probe and application thereof in Pb < 2 + > detection, and belongs to the field of chemical analysis and detection. According to the present invention, the chromophore of the benzothiazole derivative is modified by the 2-pyridine formylhydrazine, such that the new compound can specifically recognize Pb < 2 + > in the aqueous solution and the electronic smoke compound, and the powerful tool is provided for the rapid detection of the Pb < 2 + > content in the electronic smoke compound.

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 invention provides a benzothiazole derivative for detecting hydrazine, a preparation method and application thereof, and a kit for detecting hydrazine, wherein the benzothiazole derivative has a structural formula shown in Formula I: the derivative is synthesized from 2-(2-aminophenyl)benzothiazole through a series of reactions, has a maximum fluorescence emission wavelength of 640nm, has strong anti-interference ability, and has a short response time to hydrazine hydrate.

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.

A method for detecting an amine compound, the method including: bringing a specimen into contact with an isothiocyanate compound having a phenanthrenequinone skeleton; and detecting a thiazole derivative formed from an amine compound contained in the specimen and the isothiocyanate compound.

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 discloses a matrine amine thiazole derivative as well as a preparation method and application thereof, the matrine amine thiazole derivative has a structural formula as shown in Figure 1, and in the structural formula, R is any one of 4-chlorphenyl, 4-nitrophenyl, 2, 4-difluorophenyl, 4-bromophenyl, 4-methoxyphenyl, 4-phenylphenyl, naphthyl and 4-iodophenyl. The method comprises the following steps: firstly, synthesizing thiourea matrine by taking sophocarpine and thiourea as initial substrates and N, N-dimethylformamide as a solvent, and then synthesizing a series of matrine derivatives by taking thiourea matrine and alpha-bromo-R-ethyl ketone as reactants and taking ethanol as a solvent. The anti-tumor activity of the matrine derivative is enhanced, the preparation method is simple and convenient, and reaction conditions are easy to control.

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.

The present invention relates to a compound which is a thiazole derivative of formula (I) or a pharmaceutically acceptable salt thereof, wherein R<supgt;1< / supgt>, R<supgt;2< / supgt>, R<supgt;3< / supgt>, R<supgt;4< / supgt>, R<supgt;5< / supgt>, R<supgt;6< / supgt>, R<supgt;7< / supgt>, Z, L, X, m, n and p are as defined herein. The compound can be used for treating and preventing bacterial infections. The present invention also relates to combinations of compounds of formula (I) with additional active agents.

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.

The invention discloses a tripterine thiazole derivative with a structure as shown in a formula III or pharmaceutically acceptable salt thereof. R is selected from # imgabs0 # R1 and R3 which are independently selected from H, C3-C4 alkyl and halogen, and # imgabs1 # R2 and R4 are independently selected from H and C1-C4 alkyl; and n is an integer of 1-5. The tripterine thiazole derivative disclosed by the invention has an obvious inhibition effect on proliferation of various tumor cells, and the inhibition effect is obviously better than that of tripterine. The invention discloses application of the tripterine thiazole derivative or the pharmaceutically acceptable salt thereof in preparation of an Hsp90 protein inhibitor. The invention also discloses application of the tripterine thiazole derivative or the pharmaceutically acceptable salt thereof in preparation of antitumor drugs. # imgabs2 #

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 a compound selected from a novel thiazole derivative compound, its pharma- ceutically acceptable salt, its solvate or its stereoisomer, and its medical use, and provides a TGFβR1 (ALK5) inhibitor that selectively inhibits only TGFβR1 without interfering with normal TGFβ signaling, and such a novel TGFβR1 inhibitor can be used for a variety of indications, including as an anticancer agent.

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.