- Monodisperse NiPd alloy nanoparticles decorated on mesoporous graphitic carbon nitride as a catalyst for the highly efficient chemoselective reduction of α,β-unsaturated ketone compounds
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Herein, the study reported extraordinary chemoselective reduction with selectivity (>99%) by the catalytic transfer hydrogenation of various α,β-unsaturated ketones with a catalyst of NiPd alloy nanoparticles decorated on mesoporous graphitic carbon nitride (NiPd/mpg-C3N4) under mild conditions in a water/methanol medium. NiPd alloy NPs were synthesized by the reduction of metal salts in oleylamine (OAm) solution with the help of borane-tert-butylamine and then decorated on mpg-C3N4via a liquid phase self-assembly method. The NiPd/mpg-C3N4 nanocatalyst was characterized by TEM, XRD and ICP-MS. The NiPd/mpg-C3N4 nanocatalyst is a highly active catalyst for the chemoselective reduction of α,β-unsaturated ketones and all organic compounds were converted with high yield and 99% selectivity. In addition, the catalyst can be reused five times without an important loss in reaction yield. This journal is
- Bayrak, Cetin,Menzek, Abdullah,Sevim, Melike
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p. 13606 - 13612
(2020/09/07)
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- The synthesis of 4,6-diaryl-2-pyridones and their bioactivation in CYP1 expressing breast cancer cells
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As part of a programme to develop anticancer prodrugs which are activated by cytochrome P450 (CYP)1B1, a library of 4,6-diaryl-2-pyridones was synthesised in yields of 6–60% from the corresponding chalcones. A number of these derivatives showed promising antiproliferative activities in human breast cancer cell lines which express CYP1B1 and CYP1A1, while showing little toxicity towards a non-tumour breast cell line with no CYP expression. Metabolism studies provided evidence supporting the involvement of CYP1 enzymes in the bioactivation of these compounds.
- Ruparelia, Ketan C.,Lodhi, Sabahat,Ankrett, Dyan N.,Wilsher, Nicola E.,Arroo, Randolph R.J.,Potter, Gerard A.,Beresford, Kenneth J.M.
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p. 1403 - 1406
(2019/04/01)
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- Design, synthesis, and carbonic anhydrase inhibition activity of benzenesulfonamide-linked novel pyrazoline derivatives
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Carbonic anhydrases (CA, EC 4.2.1.1) are Zinc metalloenzymes and are present throughout most living organisms. Among the catalytically active isoforms are the cytosolic CA I and II, and tumor-associated CA IX and CA XII. The carbonic anhydrase (CA) inhibitory activities of newly synthesized pyrazoline-linked benzenesulfonamides 18–33 against human CA (hCA) isoforms I, II, IX, and XII were measured and compared with that of acetazolamide (AAZ), a standard inhibitor. Potent inhibitory activity against hCA I was exerted by compounds 18–25, with inhibition constant (KI) values of 87.8–244.1 nM, which were greater than that of AAZ (KI, 250.0 nM). Compounds 19, 21, 22, 29, 30, and 32 were proven to have inhibitory activities against hCA IX with KI values (5.5–37.0 nM) that were more effective than or nearly equal to that of AAZ (KI, 25.0 nM). Compounds 20–22, and 30 exerted potent inhibitory activities (KIs, 7.1–10.1 nM) against hCA XII, in comparison with AAZ (KI, 5.7 nM).
- Abdel-Aziz, Alaa A.-M.,El-Azab, Adel S.,Bua, Silvia,Nocentini, Alessio,Abu El-Enin, Mohamed A.,Alanazi, Mohammed M.,AlSaif, Nawaf A.,Hefnawy, Mohamed M.,Supuran, Claudiu T.
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p. 425 - 431
(2019/03/27)
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- NOTCH INHIBITORS FOR USE IN THE TREATMENT OF T-CELL ACUTE LYMPHOBLASTIC LEUKEMIA
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Compounds of formula (I) in the capacity of compounds with anti-tumor activity for the treatment of T-cell acute lymphoblastic leukemia (T-ALL).
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Page/Page column 25; 28
(2018/07/29)
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- A kind of compounds with analgesic effect and its preparation method (by machine translation)
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This invention relates to a kind of compounds with analgesic effect and its preparation method, the structural formula of this compound as the following I, II, III or IV is shown, wherein R is the chemical formula is C n H 2n+1 straight chain alkyl, n=1-7. The invention also discloses the above-mentioned several kinds of different structural formula of compound preparation method, the preparation of the same and the application of the capsaicin receptor inhibitors. The present invention provides the compound has strong analgesic activity, more than du Lengding part, and pharmacological experiment has not found this compound has addiction side effects. The present invention provides the compound plus pharmaceutically acceptable vector can be prepared as pharmaceutical compositions and pharmaceutical preparation, and can be developed with the addiction of preparing a medicine analgesia class. (by machine translation)
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- METHOD FOR PRODUCING LIQUIRITIGENIN PRECURSOR
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PROBLEM TO BE SOLVED: To provide a method which is suitable as a mass production method of liquiritigenin. SOLUTION: Provided is a method for producing liquiritigenin, comprising: synthesizing and crystallizing a trialkoxy-isoliquiritigenin represented by a formula (iii) by coupling a 4-alkoxycinnamic acid represented by a formula (i) and a 1,3-alkoxybenzene represented by a formula (ii) by a Friedel-Craft reaction (A); and eliminating a protective group to obtain isoliquiritigenin represented by a formula (iv). The isoliquiritigenin represented by a formula (iv) is administered in a body as a precursor of liquiritigenin represented by a formula (v), which is converted to a (-) form of liquiritigenin in the body. COPYRIGHT: (C)2016,JPOandINPIT
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Paragraph 0009
(2016/11/24)
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- Synthesis, antitubercular activity, and molecular modeling studies of analogues of isoliquiritigenin and liquiritigenin, bioactive components from Glycyrrhiza glabra
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Isoliquiritigenin (ISL, 1) and liquiritigenin (LTG, 2) were isolated from the rhizomes of Glycyrrhiza glabra. In an attempt to develop potent and selective antituberculosis agents, a series of ISL analogues were synthesized mainly via acid- and base-catalyzed Claisen-Schmidt condensation reaction for their antitubercular activity. Compared to ISL (MIC = 25 μg/mL), analogues 5, 8, and 10 showed similar antitubercular activity, but, interestingly, 6, 7, and 15 exhibited twofold higher activity (MIC = 12.5 μg/mL) over ISL, against Mycobacterium tuberculosis. Among the LTG derivatives, LTG 4′-acetate and LTG-oxime were found to be as active (MIC = 25 μg/mL) as LTG. It is the first report on antimycobacterial activity of these ISL- and LTG-based derivatives. Molecular docking and in silico ADME studies revealed that compounds 6, 7, and 15 are potent inhibitors of M. tuberculosis H37Rv alanine dehydrogenase and showed compliance with standard parameters of drug likeness.
- Gaur, Rashmi,Thakur, Jay Prakash,Yadav, Dharmendra K.,Kapkoti, Deepak Singh,Verma, Ram Kishor,Gupta, Namita,Khan, Feroz,Saikia, Dharmendra,Bhakuni, Rajendra Singh
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p. 3494 - 3503
(2015/08/03)
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- Synthesis of isobavachalcone and some organometallic derivatives
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Isobavachalcone [2′,4,4′-trihydroxy-3′-(3″-methyl- 2″-butenyl)chalcone, 1] is a prenylated chalcone that has broad biological activity, in particular against neuroblastomas, the most common cancer in infancy. It is currently commercially available at a cost of 190/mg by extraction from Psoralea corylifolia and a number of other African and Asian plants. Several synthetic routes have been explored, and the most efficient procedure involves the palladium-catalysed Stille coupling of 3-iodo-2,4-bis(methoxymethoxy)acetophenone (25) with prenyltributyltin, Claisen-Schmidt condensation with 4-(methoxymethoxy)benzaldehyde to form the triply MOM-protected prenylchalcone 27 and finally deprotection with 2 M HCl in methanol to form isobavachalcone in an overall yield of 15 % over five steps. The X-ray crystal structures of 2,4-dihydroxy-3-iodoacetophenone (21) and of several prenylated chalcones are reported, including the elucidation of their hydrogen-bonding networks in the solid state. The synthetic route has been extended to include organometallic derivatives in which the 4-(methoxymethoxy) benzaldehyde used in the Claisen-Schmidt condensation has been replaced by formylferrocene, formylruthenocene or (η5-formylcyclopentadienyl) (η4-tetraphenylcyclobutadiene)cobalt to form the corresponding analogues of isobavachalcone containing organometallic sandwich moieties.
- Grealis, John P.,Mueller-Bunz, Helge,Ortin, Yannick,Casey, Michael,McGlinchey, Michael J.
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p. 332 - 347
(2013/03/13)
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- Hierarchical mesoporous zeolites: Direct self-assembly synthesis in a conventional surfactant solution by kinetic control over the zeolite seed formation
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By kinetic control over the zeolite seed formation, we report the direct fabrication of hierarchical mesoporous zeolites using hexadecyl trimethyl ammonium bromide (CTAB) as the soft template in a conventional solution route. Nanometer-sized, subnanocrystal-type zeolite seeds with a high degree of polymerization are essential to prevent the formation of a separate amorphous mesoporous phase and the phase separation between the mesophase and zeolite crystals in the presence of CTAB and a certain amount of ethanol. The mechanisms for the formation of hierarchically porous zeolites in the solution process, including the effect of mother liquid aging, formation of subnanocrystal zeolite seeds and their self-assembly effect with CTAB, and the role of ethanol are proposed and discussed in detail. The prepared mesoporous ZSM-5 zeolite showed much higher catalytic activity than conventional counterparts for aldol condensations involving large molecules, especially in the synthesis of vesidryl.
- Zhu, Yan,Hua, Zile,Zhou, Jian,Wang, Lijun,Zhao, Jinjin,Gong, Yun,Wu, Wei,Ruan, Meiling,Shi, Jianlin
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experimental part
p. 14618 - 14627
(2012/02/03)
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- Direct synthesis of carbon-templating mesoporous ZSM-5 using microwave heating
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Carbon-templated mesoporous ZSM-5 zeolites were synthesized directly avoiding a drying process. Carbon nanoparticles were simply mixed into synthesis precursor of ZSM-5 and hydrothermally treated by microwave irradiation. The amount of mesopores formed inside the ZSM-5 single crystals was controllable by adjusting the amount of carbon used. For comparison, mesoporous ZSM-5 zeolites have also been synthesized under hydrothermal conditions. The influence of microwave irradiation on mesoporous ZSM-5 materials was thoroughly investigated by using nitrogen adsorption/desorption studies and 27Al MAS NMR. The nature of acid sites both in the micropores (internal) and on the surface of mesopores (external) was investigated by in situ FTIR spectroscopy using pyridine (Py) and 2′,6′-di-tert-butylpyridine (DTBPy) as a probe molecules. Mesoporous ZSM-5 prepared by microwave synthesis showed higher catalytic activity in the bulky molecular reaction of 2′,4′- dimethoxyacetophenone (2′,4′-DMAP) with 4-methoxybenzaldehyde as a model reaction in comparison with the results obtained over hydrothermally prepared ZSM-5. The further catalytic behavior has been studied in condensation reaction and cracking of substituted benzene.
- Koo, Jeong-Boon,Jiang, Nanzhe,Saravanamurugan, Shunmugavel,Bejblova, Martina,Musilova, Zuzana,Cejka, Jiri,Park, Sang-Eon
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experimental part
p. 327 - 334
(2011/02/27)
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- Iodine-catalyzed efficient synthesis of chalcones by grinding under solvent-free conditions
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Chalcones are useful intermediates in organic synthesis and exhibit a large number of different biological activities. Chalcones have been synthesized in high yields by Claisen-Schmidt condensation of substituted acetophenones with various aromatic aldehydes in the presence of 10 mol% of iodine at room temperature by grinding under solvent-free conditions.
- Wang, Hongshe,Zeng, June
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experimental part
p. 1209 - 1212
(2009/12/03)
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- Synthesis and antiinflammatory activity of some new 1,3,5-trisubstituted pyrazolines bearing benzene sulfonamide
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Nineteen new 2-pyrazoline bearing benzenesulfonamide derivatives were synthesized by condensing chalcones with 4-hydrazinonbenzenesulfonamide hydrochloride. Their chemical structures were proved by means of IR, 1H NMR, 13C NMR, mass spectroscopic and elemental analyses data. These compounds were tested at dose of 20 mg/kg for their anti-inflammatory activity in carrageenan-induced rat paw edema model and volume of paw edema was measured at 0, 3 and 5 h. Two compounds 3k and 3l were found to be more active than celecoxib throughout the study (at 3 and 5 h). While two other compounds 3m and 3n showed more potent activity than celecoxib at 5 h. They are devoid of ulcerogenic potential when administered orally at a dose of 60 mg/kg. Compounds (3k-m) showed COX-1 and COX-2 inhibitory activity at 0.05 μM.
- Rathish,Javed, Kalim,Ahmad, Shamim,Bano, Sameena,Alam,Pillai,Singh, Surender,Bagchi, Vivek
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scheme or table
p. 255 - 258
(2009/05/07)
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- A Novel α-Hydroxydihydrochalcone from the Heartwood of Pterocarpus angolensis D.C.: Absolute Configuration, Synthesis, Photochemical Transformations, and Conversion into α-Methyldeoxybenzoins
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The absolute configuration of (αR)-α,2'-dihydroxy-4,4'-dimethoxydihydrochalcone from the heartwood of Pterocarpus angolensis D.C. is established.Its structure is substantiated by synthesis and by photochemical conversion of its α-O-tosyl derivative into an α-tosyloxymethyldeoxybenzoin and hence to the α-methyldeoxybenzoin analogue.The photochemical step also leads, amongst others, to α-hydroxymethyldeoxybenzoin, β-hydroxydihydrochalcone, and 2-benzylbenzofuran-3-one analogues depending on the conditions the photolysis.
- Bezuidenhoudt, Barend C. B.,Brandt, E. Vincent,Roux, David G.
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p. 263 - 269
(2007/10/02)
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