- Quinazoline derivative and preparation method and application thereof
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The invention discloses a novel compound 4-(3 '-R substituted-5'-R substituted-4 '-hydroxyanilino) quinazoline derivative and a preparation method and application thereof. The structural formulas of the compound are shown as formulas I and II. The compound has good activity of preventing and treating chicken coccidiosis and can be used as a therapeutic agent for preventing and treating chicken coccidiosis in the field of preparation of medicines for preventing and treating chicken coccidiosis.
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- Pyridazinone derivative and application thereof
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The invention provides a pyridazinone derivative and an application thereof, the pyridazinone derivative with the structure shown in the formula (I) provided by the invention has good activity as a thyroid hormone beta receptor agonist by selecting a specific modification group. The compound can be used for treating and/or preventing diseases caused by thyroid hormone regulation.
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Paragraph 0298-0303
(2020/11/23)
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- Substituted pteridinones as p90 ribosomal S6 protein kinase (RSK) inhibitors: A structure-activity study
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The activity of p90 ribosomal S6 kinase 2 (RSK2) has emerged as an attractive target for cancer therapy due to its role in the regulation of diverse cellular processes, such as cell transformation and proliferation. Several pan-RSK inhibitors have been identified with BI-D1870 and the pseudo-analogs LJH685 and LJI308 being the most selective, potent, and frequently used small molecule inhibitors. We designed and synthesized a series of pteridinones and pyrimidines to evaluate the structural features of BI-D1870 that are required for RSK2 inhibition. We have identified inhibitors of RSK2 activity, evaluated their target engagement in cells, and measured their effect on cell viability and cytotoxicity in the MOLM-13 acute myeloid leukemia (AML) cell line. The results of our studies support that RSK2 inhibition can be achieved in MOLM-13 cells without potent cytotoxicity. The structure-activity data from this study will be used as a platform to develop novel RSK2 inhibitors.
- Backos, Donald S.,Casalvieri, Kimberly A.,Matheson, Christopher J.,Reigan, Philip
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- Synthesis and some transformations of polybrominated quinone diazides
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The reduction of polybrominated o- and p-nitrophenols with granular tin in concentrated aqueous HCl gave polybrominated aminophenols which were diazotized with sodium nitrite in concentrated sulfuric acid at 0°C to obtain polybrominated o- and p-quinone diazides. Their thermolysis with elimination of nitrogen generated ketocarbenes which reacted with acetylacetone to form insertion products at the activated methylene group. Ketocarbenes generated from o-quinone diazides reacted with typical dipolarophiles such as acetonitrile, benzonitrile, styrene, and phenylacetylene to afford the corresponding [3 + 2]-cycloaddition products.
- Vasin,Fadin,Tarasova
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p. 1815 - 1821
(2018/02/06)
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- A simple protocol for the visual discrimination of natural cyclodextrins in aqueous solution using perichromic probes
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(Graph Presented) Three synthesized compounds, 4-(4-nitrostyryl)phenol, 2,6-dibromo-4-(2,4-dinitrobenzylideneamino) phenol and 2,6-dichloro-4-(2,4-dinitrobenzylideneamino)phenol, were deprotonated to generate the perichromic dyes 2b, 3b and 4b, respectively. These dyes were used as probes to investigate the micropolarity of natural cyclodextrins (CyDs) and it was observed that they interact differently with the CyDs according to the molecular structure of the dye and the diameter of the CyD. The solvatochromic bands of the dyes that interacted with the CyDs were bathochromically shifted, suggesting that the probes were transferred to the hydrophobic interior of the CyD in aqueous solution. Dyes 2b and 4b were found to be very selective for α-CyD and γ-CyD, respectively, while β- and γ-CyD changed the color of the solution of compound 3b. These dyes were then successfully used in a simple assay that allows the naked-eye discrimination of natural CyDs in aqueous solution, without the need for expensive techniques.
- Nandi, Leandro G.,Nicoleti, Celso R.,Stock, Rafaela I.,Barboza, Tainá A.,Andreaus, Jürgen,Machado, Vanderlei G.
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p. 1600 - 1606
(2015/02/19)
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- Efficient reducing system based on iron for conversion of nitroarenes to anilines
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Reduction of nitroarenes with low solubility in EtOH-H2O to anilines easily occurs in a Fe-NH4Cl-acetone-H2O system, and treatment of the same nitroarenes with Fe-NH4Cl-EtOH-H2O hardly furnished the corresponding products. Under the reaction condition, the reducible or hydrolysable groups are not affected.
- Xiao, Zhu-Ping,Wang, Ying-Chun,Du, Gao-Yu,Wu, Jun,Luo, Tao,Yi, Shou-Fu
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experimental part
p. 661 - 665
(2011/03/19)
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- NOVEL PHARMACEUTICAL COMPOSITIONS
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The invention provides the use of compounds of formula (I) or pharmaceutically acceptable esters, amides, solvates or salts thereof, including salts of such esters or amides, and solvates of such esters, amides or salts, for the manufacture of a medicament for the treatment or prophylaxis of a condition that may be treated with a thyroid receptor agonist or partial agonist wherein R1, R2, R3, R4, Y, W and R5 are as defined in the specification. The invention also provides compounds of formula (Ia) or pharmaceutically acceptable esters, amides, solvates or salts thereof, including salts of such esters or amides, and solvates of such esters, amides or salts, formula (Ia) wherein R1, R2, R3, R4, Y, W and R5 are as defined in the specification.
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Page/Page column 51-52
(2008/06/13)
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- THYROID RECEPTOR AGONISTS
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The invention provides compounds of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition mediated by a thyroid receptor. Formula (I), wherein R1, R2, n, Y, Y', R3, R4, W and R5 are as defined in the specification.
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Page/Page column 64-65
(2010/02/14)
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- Hair colouring and conditioning compositions
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A hair colouring and conditioning composition comprising: (a) a hair colouring agent; and (b) a hair conditioning agent; wherein the composition provides an Average Combing Index Value of greater than 1.2 as measured by the Combing Technical Test Method. The products can provide excellent hair colouring together with excellent conditioning, reduced hair damage, brittleness and dryness, and is convenient and easy to use.
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- Hair conditioning compositions and their use in hair colouring compositions
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The present invention relates to a hair care composition comprising a aminofunctional polysiloxane having a specified average effective particle size which provides improved durable conditioning particularly when utilised in conjunction with a hair colouring composition.
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