- 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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Read Online
- (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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- 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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- Structure-guided, single-point modifications in the phosphinic dipeptide structure yield highly potent and selective inhibitors of neutral aminopeptidases
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Seven crystal structures of alanyl aminopeptidase from Neisseria meningitides (the etiological agent of meningitis, NmAPN) complexed with organophosphorus compounds were resolved to determine the optimal inhibitor-enzyme interactions. The enantiomeric phosphonic acid analogs of Leu and hPhe, which correspond to the P1 amino acid residues of well-processed substrates, were used to assess the impact of the absolute configuration and the stereospecific hydrogen bond network formed between the aminophosphonate polar head and the active site residues on the binding affinity. For the hPhe analog, an imperfect stereochemical complementarity could be overcome by incorporating an appropriate P1 side chain. The constitution of P1′-extended structures was rationally designed and the lead, phosphinic dipeptide hPhePψ[CH2]Phe, was modified in a single position. Introducing a heteroatom/heteroatom-based fragment to either the P1 or P1′ residue required new synthetic pathways. The compounds in the refined structure were low nanomolar and subnanomolar inhibitors of N. meningitides, porcine and human APNs, and the reference leucine aminopeptidase (LAP). The unnatural phosphinic dipeptide analogs exhibited a high affinity for monozinc APNs associated with a reasonable selectivity versus dizinc LAP. Another set of crystal structures containing the NmAPN dipeptide ligand were used to verify and to confirm the predicted binding modes; furthermore, novel contacts, which were promising for inhibitor development, were identified, including a π-π stacking interaction between a pyridine ring and Tyr372.
- Vassiliou, Stamatia,W?glarz-Tomczak, Ewelina,Berlicki,Pawe?czak, Ma?gorzata,Nocek, Bogus?aw,Mulligan, Rory,Joachimiak, Andrzej,Mucha, Artur
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p. 8140 - 8151
(2014/12/10)
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- Design, synthesis, and biological evaluation of 17-cyclopropylmethyl-3, 14β-dihydroxy-4,5α-epoxy-6β-[(4′-pyridyl)carboxamido] morphinan derivatives as peripheral selective μ opioid receptor agents
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Peripheral selective μ opioid receptor (MOR) antagonists could alleviate the symptoms of opioid-induced constipation (OIC) without compromising the analgesic effect of opioids. However, a variety of adverse effects were associated with them, partially due to their relatively low MOR selectivity. NAP, a 6β-N-4′-pyridyl substituted naltrexamine derivative, was identified previously as a potent and highly selective MOR antagonist mainly acting within the peripheral nervous system. The noticeable diarrhea associated with it prompted the design and synthesis of its analogues in order to study its structure-activity relationship. Among them, compound 8 showed improved pharmacological profiles compared to the original lead, acting mainly at peripheral while increasing the intestinal motility in morphine-pelleted mice (ED50 = 0.03 mg/kg). The slight decrease of the ED50 compared to the original lead was well compensated by the unobserved adverse effect. Hence, this compound seems to be a more promising lead to develop novel therapeutic agents toward OIC.
- Yuan, Yunyun,Elbegdorj, Orgil,Chen, Jianyang,Akubathini, Shashidhar K.,Zhang, Feng,Stevens, David L.,Beletskaya, Irina O.,Scoggins, Krista L.,Zhang, Zhenxian,Gerk, Phillip M.,Selley, Dana E.,Akbarali, Hamid I.,Dewey, William L.,Zhang, Yan
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p. 10118 - 10129
(2013/01/16)
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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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