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41661-47-6Relevant articles and documents
Ligand-based rational design, synthesis and evaluation of novel potential chemical chaperones for opsin
Bassetto, Marcella,Brancale, Andrea,Pasqualetto, Gaia,Pileggi, Elisa,Rozanowska, Malgorzata,Schepelmann, Martin,Varricchio, Carmine
supporting information, (2021/09/24)
Inherited blinding diseases retinitis pigmentosa (RP) and a subset of Leber's congenital amaurosis (LCA) are caused by the misfolding and mistrafficking of rhodopsin molecules, which aggregate and accumulate in the endoplasmic reticulum (ER), leading to photoreceptor cell death. One potential therapeutic strategy to prevent the loss of photoreceptors in these conditions is to identify opsin-binding compounds that act as chemical chaperones for opsin, aiding its proper folding and trafficking to the outer cell membrane. Aiming to identify novel compounds with such effect, a rational ligand-based approach was applied to the structure of the visual pigment chromophore, 11-cis-retinal, and its locked analogue 11-cis-6mr-retinal. Following molecular docking studies on the main chromophore binding site of rhodopsin, 49 novel compounds were synthesized according to optimized one-to seven-step synthetic routes. These agents were evaluated for their ability to compete for the chromophore binding site of opsin, and their capacity to increase the trafficking of the P23H opsin mutant from the ER to the cell membrane. Different new molecules displayed an effect in at least one assay, acting either as chemical chaperones or as stabilizers of the 9-cis-retinal-rhodopsin complex. These compounds could provide the basis to develop novel therapeutics for RP and LCA.
TEAD INHIBITORS AND USES THEREOF
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Paragraph 00465; 00813, (2020/12/11)
The present invention provides compounds, compositions thereof, and methods of using the same.
Synthesis and characterization of piperidin-4-one derivatives using green solvent
Hemalatha,Ilangeswaran
, p. 981 - 984 (2020/03/24)
A deep eutectic solvent of glucose-urea was found to be an inexpensive and effective reaction medium in the synthesis of piperidin-4-one derivatives. In this work, 3-methyl-2,6-diphenyl piperidin-4-one (4a), 3,5-dimethyl-2,6-diphenylpiperidin-4-one (4b), 2,6-diphenylpiperidin-4-one (4c), piperidin-4-one (4d), 3,5-dimethylpiperidin-4-one (4e), 3-methyl-2,6-di(2-hydroxyphenyl)piperidin-4-one (4f), 3,5-dimethyl 2,6-di(2-hydroxyphenyl)piperidin-4one (4g) were synthesized using a deep eutectic solvent (DES) of glucose and urea with the percentage composition of 60:40. The yields of these products were 82, 78, 75, 68, 72, 70 and 70 %, respectively. The products obtained were characterized by FT-IR and 1H NMR spectroscopic techniques. A synthesis of piperidin-4-one derivatives by using this green solvent was considered to be new environmentally safe synthetic method.
Iron-catalyzed oxidative functionalization of C(sp3)-H bonds under bromide-synergized mild conditions
Yu, Han,Zhao, Qixin,Wei, Zheyu,Wu, Zhikang,Li, Qi,Han, Sheng,Wei, Yongge
supporting information, p. 7840 - 7843 (2019/07/12)
An efficient oxidation and functionalization of C-H bonds with an inorganic-ligand supported iron catalyst and hydrogen peroxide to prepare the corresponding ketones was achieved using the bromide ion as a promoter. Preliminary mechanistic investigations indicated that the bromide ion can bind to FeMo6 to form a supramolecular species (FeMo6·2Br), which can effectively catalyze the reaction.
Synthesis method of intermediate 4-piperidone
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Paragraph 0022-0056, (2019/12/02)
The invention discloses a synthesis method of an intermediate 4-piperidone. The method comprises the following steps: adding beta-alanine methyl ester into ethanol, placing the raw material into a reaction kettle, adding ethylene, uniformly mixing the raw materials, cooling the raw materials to 0-10 DEG C, adding a catalyst aid and sodium ethoxide, stirring the raw materials for reaction, and cooling a reaction product to room temperature after the reaction is finished; and performing reduced pressure distillation to remove ethanol; adding DMF into a reaction kettle, uniformly stirring and mixing the components, heating the mixture to 110-130 DEG C, and carrying out reflux reaction under a stirring condition for 1-2 hours; cooling the reaction product to room temperature, extracting the reaction product with ethyl acetate, performing evaporation to remove ethyl acetate, and carrying out reduced pressure distillation to obtain the 4-piperidone. The synthesis method disclosed by the invention adopts a one-pot method, does not need an intermediate purification step, reduces resource waste, is simple to operate, short in production process, high in raw material conversion rate and relatively low in production cost, and has relatively high economic benefits.
Synthesis method of bacterial infection resistant medicine intermediate
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, (2018/07/30)
The invention belongs to the technical field of chemical medicine intermediate synthesis, and particularly relates to a synthesis method of a bacterial infection resistant medicine intermediate. Liquid ammonia and acrylic ester are used as raw materials for preparing a diester type secondary amine compound 1; then, through cyclization, piperidone is prepared; then, scientific reaction catalysts, temperature and time are used; substitution reaction of secondary amine and iso-propyl iodide is used; the target product is synthesized through six-step reaction; the yield of the whole route reachesup to 35 percent.
Compound used as ALK (anaplastic lymphoma kinase) inhibitor and application thereof
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Paragraph 0284; 0286; 0287, (2018/11/04)
The invention discloses a compound shown in a formula I, and pharmaceutically acceptable salts, stereoisomers, solvates or predrugs. The symptoms are defined in claim requirements. The compound shownin the formula I has good inhibiting activity on ALK (anaplastic lymphoma kinase), and can be used for preparing medicines for adjusting the activity of the ALK activity or treating the ALK-related diseases, especially nonsmall-cell lung cancer drugs. (The formula I is shown in the attached figure.).
Synthesis and characterization of Co3O4 immobilized on dipeptide-functionalized silica-coated magnetite nanoparticles as a catalyst for the selective aerobic oxidation of alcohols
Khodaei, Mohammad Mehdi,Dehghan, Mahsa
, p. 11381 - 11389 (2018/07/24)
Synthesis and characterization of a new silica-coated magnetite nanocatalyst are described. This catalyst was prepared through a multistep procedure consisting of surface modification, functionalization with the product of an Ugi multicomponent reaction, and immobilization of Co3O4 on silica-coated magnetite nanoparticles. The prepared nanocatalyst was characterized using various techniques such as Fourier-transform infrared and energy-dispersive X-ray spectroscopies, thermal and elemental analyses, X-ray diffraction, and field-emission scanning and transmission electron microscopies. The catalyst showed high catalytic activity for the aerobic oxidation of alcohols in acetonitrile as the solvent at mild temperatures and reusability for five repeated runs without loss of its activity.
IMMUNOREGULATORY AGENTS
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Paragraph 0298, (2016/06/01)
Compounds that modulate the oxidoreductase enzyme indoleamine 2,3- dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.
Synthesis and antiproliferative activity of cyclic arylidene ketones: a direct comparison of monobenzylidene and dibenzylidene derivatives
Huber, Imre,Zupk, Istvn,Kovcs, Ida J.,Minorics, Renta,Gulys-Fekete, Gergely,Masz, Gbor,Perjsi, Pl
, p. 973 - 981 (2015/02/19)
Abstract To give further insight into the influence of the structural modifications of enones and dienones on their antiproliferative properties, 25 derivatives of enones: (E)-2-benzylidene-1-cyclohexanones, (E)-2-benzylidene-1-tetralones, (E)-2-benzylidene-1-indanone, and dienones: (E,E)-2,5- or 2,6-dibenzylidene-1-cyclanones, (E,E)-3,5-dibenzylidene-4-piperidones were synthesized using a newly developed "one-pot" synthetic method. Due to the fact that all of them have the same aryl substituents (phenyl or 4-chlorophenyl) in the arylidene moiety, it is possible to compare the relevant contribution of the single-point structural modifications (type of ring or N-substitution) on their potency on the basis of their IC 50 values. Their antiproliferative activity was evaluated against the following four human adherent cancer cell lines: HeLa, A431, A2780, and MCF7. The cytotoxicity screen has revealed that the dibenzylidene dienones in general dominate the monobenzylidene enones in this respect. The nitrogen-containing heterocyclic dienones at the same time displayed higher inhibitory properties toward these human carcinoma cell lines compared with their homocyclic dienone analogs. One of the eight newly prepared 4-piperidone derivatives, N-(γ-oxobutyl)-(E,E)-3,5-bis(p-chlorobenzylidene)-4-piperidone is as potent a cell growth inhibitor (IC 50 of 0.438-1.409 μM) as the N-methyl-(E,E)-3,5-bis(p-chlorobenzylidene)-4-piperidone (IC 50 of 0.447-1.048 μM), one of the most active among the previously described compounds in this series. Catalytic hydrogen-transfer isomerization of compounds with two exocyclic benzylidene double bonds to derivatives with endocyclic double bonds results in the complete loss of antiproliferative activity. The structural modifications and 50 % inhibitory concentration (IC 50) values resulted in correlations which can promote the design of more potent derivatives of the 4-piperidone dienones.