- 3, 5-disubstituted hydantoin compound as well as preparation method and application thereof
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The invention provides a 3, 5-disubstituted hydantoin compound as well as a preparation method and an application thereof. The structure of the compound is shown in formula I in the description. The application of the 3, 5-disubstituted hydantoin compound shown in the formula I or solvates, hydrates or salts of the compound in preparation of medicines for treating Alzheimer's disease, vascular dementia and other dementia diseases with memory impairment also belongs to the protection scope. Animal experiments prove that the compound has the effect of saving memory of animal models, has high safety, does not have mutagenicity, can stay in blood for several hours after oral administration and intravenous injection, and can enter the brain.
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- Discovery of Inhibitor of Wnt Production 2 (IWP-2) and Related Compounds As Selective ATP-Competitive Inhibitors of Casein Kinase 1 (CK1) δ/?
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Inhibitors of Wnt production (IWPs) are known antagonists of the Wnt pathway, targeting the membrane-bound O-acyltransferase porcupine (Porcn) and thus preventing a crucial Wnt ligand palmitoylation. Since IWPs show structural similarities to benzimidazol
- García-Reyes, Balbina,Witt, Lydia,Jansen, Bj?rn,Karasu, Ebru,Gehring, Tanja,Leban, Johann,Henne-Bruns, Doris,Pichlo, Christian,Brunstein, Elena,Baumann, Ulrich,Wesseler, Fabian,Rathmer, Bernd,Schade, Dennis,Peifer, Christian,Knippschild, Uwe
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supporting information
p. 4087 - 4102
(2018/05/23)
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- MLKL INHIBITORS
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Purine derivatives that inhibit cellular necroptosis and/or human MLKL, pharmaceutical compositions thereof, and methods of treating an MLKL-mediated disorder with an effective amount of the compound or composition. Said MLKL-mediated disorder is pathology associated necroptosis, including ischemia-reperfusion damage, neurodegeneration, and inflammatory diseases such as acute pancreatitis, multiple sclerosis, inflammatory bowel disease, and allergic colitis.
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Paragraph 0361-0362
(2018/09/26)
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- 4-oxo-alkylated tetramic acid compounds and preparation method thereof
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The invention relates to novel compounds and a preparation method thereof. The general structural formula is shown as formula I in the description. Animal experiments prove that the compounds have the effect of saving memories of animal models, are high in safety, have no mutagenicity, can remain in blood for hours after oral administration and intravenous injection, can enter brains and can be used for preparing drugs for treating diseases such as Alzihemer's disease, Parkinson's disease, Huntington's disease, vascular dementia, schizophrenia, autism and the like.
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- 4-oxo-alkylated tetramic acid compound as well as preparation method and application thereof
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The invention relates to a novel compound as well as preparation method and application thereof. The structural formula of the novel compound is as shown in a formula I. Animal tests show that the compound provided by the invention has a memory effect of rescuing animal models, is high in security and free of mutagenicity induction, can be retained for hours in blood after oral taking and intravenous injection, can be fed into brains and can be used for preparing medicines for treating senile dementia, Parkinsonism, Huntington diseases, vascular dementia, schizophrenia, autism and the like.
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- One-Step Synthesis of Substituted Benzofurans from ortho- Alkenylphenols via Palladium-Catalyzed C=H Functionalization
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A dehydrogenative oxygenation of C(sp2)=H bonds with intramolecular phenolic hydroxy groups has been developed, which provides a straightforward and concise access to structurally diversely benzofurans from ortho-alkenylphenols. The reaction is catalyzed by palladium on carbon (Pd/C) without any oxidants and sacrificing hydrogen acceptors.
- Yang, Dejun,Zhu, Yifei,Yang, Na,Jiang, Qiangqiang,Liu, Renhua
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supporting information
p. 1731 - 1735
(2016/06/09)
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- Synthesis and in vitro antibacterial activity of gemifloxacin derivatives containing a substituted benzyloxime moiety
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A series of novel gemifloxacin (GMFX) derivatives containing a substituted benzyloxime moiety with remarkable improvement in lipophilicity were synthesized. The target compounds evaluated for their in vitro antibacterial activity against representative strains. Our results reveal that most of the target compounds have considerable potency against all of the tested Gram-positive strains including MRSA and MRSE (MIC: 90: 1 μg/mL) is 8-fold more active than GMFX, and 2-fold more active than GMFX and moxifloxacin against MRSE clinical isolates (MIC90: 4 μg/mL). Crown Copyright
- Feng, Lianshun,Lv, Kai,Liu, Mingliang,Wang, Shuo,Zhao, Jing,You, Xuefu,Li, Sujie,Cao, Jue,Guo, Huiyuan
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p. 125 - 136
(2012/11/07)
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- Synthesis and biological activity of pyridopyridazin-6-one p38α MAP kinase inhibitors. Part 2
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This manuscript concludes the Structure Activity Relationship (SAR) on the pyridazinone scaffold and identifies a compound with subnanomolar p38α activity and 24 h coverage in the rat arthritis efficacy model.
- Tynebor, Robert M.,Chen, Meng-Hsin,Natarajan, Swaminathan R.,O'Neill, Edward A.,Thompson, James E.,Fitzgerald, Catherine E.,O'Keefe, Stephen J.,Doherty, James B.
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p. 5971 - 5975
(2012/11/07)
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- Synthesis of benzyl bromides with hexabromoacetone: An alternative path to drug intermediates
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A series of benzyl bromides were efficiently prepared from the corresponding alcohols with Br3CCOCBr3/PPh3 at low temperatures and under neutral conditions. The present protocol was applied to the heterocyclic analogues and to the successful synthesis of the precursor of the antiulcer drug omeprazole, thus furnishing an alternate, mild method for the preparation of these drug intermediates. A significant steric factor was observed throughout both series supporting a SN2 mechanism.
- Joseph, Kara M.,Larraza-Sanchez, Isabel
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experimental part
p. 13 - 16
(2011/02/25)
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- CARBON-ISOTOPE MONOXIDE LABELING OF DAA1106 AND ITS ANALOGUES TO BE USED AS TRACERS FOR A PERIPHERAL TYPE BENZODIAZEPINE BINDING SITE
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A potent and selective ligand for peripheral benzodiazepine receptor (PBR), N-(2,5-dimethoxybenzyl)-N-(5-fluoro-2-phenoxyphenyl)acetamide or DAA1106 and eight structurally related analogues were labelled with 11C at carbonyl position of the mol
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Page/Page column 43-44
(2010/11/26)
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- Synthesis of N-(2,5-dimethoxybenzyl)-N-(5-fluoro-2-phenoxyphenyl)[carbonyl- 11C]acetamide ([carbonyl- 11C]DAA1106) and analogues using [11C]carbon monoxide and palladium(0) complex
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N-(2,5-Dimethoxybenzyl)-N-(5-fluoro-2-phenoxyphenyl)acetomide (DAA1106), a potent and selective ligand for peripheral benzodiazepine receptor, and eight structurally related analogues were labelled with 11C at the carbonyl position using a low
- Rahman, Obaidur,Langstroem, Bengt
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p. 1192 - 1199
(2008/04/05)
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- Total synthesis of racemosol and de-O-methylracemosol, potent cyclooxygenase (COX) inhibitors and antimalarial agents
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The total synthesis of antimalarial and cyclooxygenase inhibitors, racemosol and de-O-methylracemosol, is described. The key steps involved the lateral lithiation reaction of ortho-methyl tolulate and the pyran formation via a tandem demethylation-cycliza
- Sae-Lao, Patcharaporn,Kittakoop, Prasat,Rajviroongit, Shuleewan
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p. 345 - 348
(2007/10/03)
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- NOVEL HETEROCYCLIC COMPOUNDS AS HSP90-INHIBITORS
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Novel heterocyclic compounds are described and demonstrated to have utility as Heat Shock Protein 90 (HSP90) inhibiting agent. Method of synthesis and use of such compounds are also described.
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Page/Page column 321
(2008/06/13)
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- Synthesis of macrocyclic ditopic receptors designed for simulataneous binding of alkaline and transition metal cations
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The synthesis of diazatetraoxacyclooctadecane derivatives bearing two catechol groups was achieved in good yield. The binucleating ligands were designed to bind both soft and hard cations simultaneously.
- Graf, Ernest,Hosseini, Mir Wais,Ruppert, Romain
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p. 7779 - 7782
(2007/10/02)
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- Tolerizing and desensitizing compounds, compositions and methods of treatment against dermatological conditions caused by allergens from plants and trees of the Anacardiaceae and Ginkgoaceae families
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Compounds, compositions and a method of treatment to tolerize and desensitize mammals sensitive to the allergenic moities found in plants of the Anacardiaceae and Ginkgoaceae families comprising the reaction product of poison ivy urushiol, poison oak urushiol, poison sumac urushiol & mixtures thereof, 3-n-alkane substituted catechol derivatives having 11 to 19 carbon atoms and the unsaturated olefinic congeners thereof with an acyl ester functioning group esterifying the catecholic hydroxy constituents of the aforementioned compounds or cell membrane residues.
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- Synthesis and antiallergenic properties of 3-n-pentadecyl- and 3-n-heptadecylcatechol esters
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A synthetic procedure is described for the preparation of 3-n-pentadecyl- and 3-n-heptadecylcatechols and their acetate and alaninate esters. The Wittig reagent prepared from 2,3-dimethoxybenzyltriphenylphosphonium bromide (III) was coupled with 1-tetrade
- Elsohly,Benigni,Torres,Watson
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p. 792 - 795
(2007/10/02)
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- A SIMPLIFIED ISOQUINOLINE SYNTHESIS
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A simple variation of the Pomeranz-Fritsch cyclization provides a short, efficient route to isoquinolines.Treatment of benzylic halides or mesylates 1 with the sodium anion of N-tosyl aminoacetaldehyde dimethyl acetal (2) followed by acid-catalyzed cyclization provides an effective, two-step preparation of isoquinolines 4.
- Boger, Dale L.,Brotherton, Christine E.,Kelley, Marshall D.
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p. 3977 - 3980
(2007/10/02)
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