- (E)-3-heteroaromatic propyl-2-enoic acid derivative as well as preparation and application thereof
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The invention relates to a (E)-3-heteroaromatic propyl-2-enoic acid derivative, and also relates to a preparation method and pharmaceutical application thereof. The compound is a novel Nrf2 activatorand has the effects of resisting oxidative stress, resisting neuritis and enhancing mitochondrial functions and biogenesis by effectively activating an Nrf2 signal path, so that nerve cells are protected, and the compound can be used for treating neurodegenerative diseases and cerebral apoplexy. In addition, the novel Nrf2 activator can also be used to treat autoimmune diseases, diabetes and nephropathy, and other chronic diseases.
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Paragraph 0054-0056
(2020/09/10)
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- Uranyl-Organic Coordination Compounds Incorporating Photoactive Vinylpyridine Moieties: Synthesis, Structural Characterization, and Light-Induced Fluorescence Attenuation
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The fluorescence of uranyl originated from electronic transitions (S11-S00 and S10-S0v, v = 0-4) of the ligand-to-metal charge transfer (LMCT) process is an intrinsic property of many uranyl coordination compounds. However, light-induced regulation on fluorescence features of uranyl hybrid materials through photoactive functional groups is less investigated. In this work, the photoactive vinyl group-containing ligands, (E)-methyl 3-(pyridin-4-yl)acrylate and (E)-methyl 3-(pyridin-3-yl)acrylate, have been used in the construction of uranyl coordination polymers in the presence of 1,10-phenanthroline (phen). Five compounds (UO2)3(μ3-O)(μ2-OH)2(L1)2(phen)2(1), (UO2)3(μ3-O)(μ2-OH)3(L1)(phen)2 (2), (UO2)3(μ3-O)(μ2-OH)3(L2)(phen)2 (3), [(UO2)2(μ2-OH)2(L2)2(phen)2]·2H2O (4), and (UO2)Zn(SO4)(phen)(H2O)(OH)2(5) were obtained under hydrothermal conditions. Compounds 1-4 are polynuclear uranyl structures with abundant π-π interactions and hydrogen bonds contributed to the 3D crystal packing of them. As model compounds, 1 and 3 are selected for exploring photoresponsive behaviors. The emission intensities of these two compounds are found to decrease gradually over the exposure time of UV irradiation. X-ray single crystal structural analysis suggests that the fluorescence attenuation can be explained by the slight rotation of pyridinyl groups around the carbon-carbon double bond during UV irradiation, which is accompanied by the change of weak interactions, i.e., π-π interactions and hydrogen bonds in strength and density. This feature of light-induced fluorescence attenuation may enable these two compounds to act as potential photoresponsive sensor materials.
- Wu, Si,Mei, Lei,Li, Fei-Ze,An, Shu-Wen,Hu, Kong-Qiu,Nie, Chang-Ming,Chai, Zhi-Fang,Shi, Wei-Qun
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supporting information
p. 14772 - 14785
(2018/11/23)
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- Synthesis of olefins via a Wittig reaction mediated by triphenylarsine
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An arsine-mediated Wittig reaction for the synthesis of olefins is described. After heating triphenylarsine in the presence of an activated alkyl bromide for 30?min, the resulting arsonium salt condensed with aldehydes in as little as 5?min at room temperature, yielding the olefins in high yields. Aromatic, heteroaromatic, and alkyl aldehydes were all suitable substrates for this process.
- Li, Lun,Stimac, Jared C.,Geary, Laina M.
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supporting information
p. 1379 - 1381
(2017/03/17)
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- Metal nanoparticle catalyzed cyclobutane cleavage reaction
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The pyridine substituted cyclobutane cleavage reaction can be catalyzed directly by the high surface energy of metallic silver/gold nanoparticles.
- Chen, Dengtai,Han, Xijiang,Jin, Wen,Zhang, Bin
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p. 100722 - 100724
(2015/12/05)
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- NRF2 REGULATORS
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The present invention relates to bis aryl analogs, pharmaceutical compositions containing them and their use as Nrf2 regulators.
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Page/Page column 158; 159
(2015/07/07)
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- A supramolecular protecting group strategy introduced to the organic solid state: Enhanced reactivity through molecular pedal motion
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A supramolecular protecting group strategy has been applied to achieve solid-state photodimerizations of olefins lined with a combination of hydrogen-bond-donor and -acceptor groups. Esters were used as protecting groups to generate head-to-head photodime
- Elacqua, Elizabeth,Kaushik, Poonam,Groeneman, Ryan H.,Sumrak, Joseph C.,Bucar, Dejan-Kresimir,MacGillivray, Leonard R.
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supporting information; experimental part
p. 1037 - 1041
(2012/02/16)
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- Development of tryptase inhibitors derived from thalidomide
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A novel series of tryptase inhibitors with a N-phenylphthalimide skeleton structurally derived from thalidomide (1) has been developed. Structure-activity relationship studies led to a potent and selective tryptase inhibitor, 2-(4-cyanophenyl)isoindole-1,3-dione-5-yl 3-(2-aminopyridin-5-yl)propanoate (7), with the IC50 value of 78 nM.
- Tetsuhashi, Masashi,Ishikawa, Minoru,Hashimoto, Mariko,Hashimoto, Yuichi,Aoyama, Hiroshi
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experimental part
p. 5323 - 5338
(2010/09/15)
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- Efficient heterogeneous palladium-montmorillonite catalysts for heck coupling of aryl bromides and chlorides
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New palladium catalysts were prepared using ion exchange or intercalation of Pd species into montmorillonite. The catalysts promote Heck reaction of various aromatic halides including aryl chlorides to give coupling products in high yields at low catalyst ratios down to 0.001 mol%. Georg Thieme Verlag Stuttgart.
- Molnár, árpád,Papp, Attila
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p. 3130 - 3134
(2008/02/13)
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- Design and synthesis of thrombin inhibitors: Analogues of MD-805 with reduced stereogenicity and improved potency
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Mitsubishi's MD-805, a potent and selective inhibitor of thrombin which contains four stereogenic centers, has been the starting point for an optimization program. A systematic synthetic study resulted in thrombin inhibitors achiral at P2 and P3 but with
- Brundish, Derek,Bull, Alice,Donovan, Vera,Fullerton, Joseph D.,Garman, Sheila M.,Hayler, Judy F.,Janus, Diana,Kane, Peter D.,McDonnell, Mark,Smith, Garrick P.,Wakeford, Robert,Walker, Clive V.,Howarth, Graham,Hoyle, William,Allen, Mark C.,Ambler, John,Butler, Keith,Talbot, Mark D.
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p. 4584 - 4603
(2007/10/03)
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- Substituted dibenzoxazepine compounds, pharmaceutical compositions and methods for treating pain
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The present invention provides substituted dibenzoxazepine compounds of Formula I: STR1 which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
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