- MACROCYCLIC COMPOUNDS
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The present invention relates to macrocyclic compounds which are capable of selective binding to a target saccharide (e.g. glucose), making them particularly well suited for use in saccharide sensing applications. The present invention also relates to processes for the preparation of said compounds, to compositions and devices comprising them, and to their use in the detection of a target saccharide.
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Paragraph 00376; 00377; 00378; 00379
(2018/10/19)
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- Regioselective nitration of anilines with Fe(NO3)3·9H2O as a promoter and a nitro source
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An efficient Fe(NO3)3·9H2O promoted ortho-nitration reaction of aniline derivatives has been developed. This reaction may go through a nitrogen dioxide radical (NO2) intermediate, which is generated by the thermal decomposition of iron(iii) nitrate. The practicality of the present method using nontoxic and inexpensive iron reagents has been shown by the broad substrate scope and applications.
- Gao, Yang,Mao, Yuanyou,Zhang, Biwei,Zhan, Yingying,Huo, Yanping
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p. 3881 - 3884
(2018/06/08)
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- SalenZn-bridged D-π-A dyes for dye-sensitized solar cells
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A series of SalenZn based dyes with triphenylamine derivatives as the donor, benzoic acid as the acceptor, and coplanar Salen complexes as the spacer have been designed and synthesized for dye-sensitized solar cells. The absorption, electrochemical, and photovoltaic properties for all sensitizers have been systematically investigated. When the tail length of the alkyl substituents is increased from C-0 to C-8 on the donor part, the efficiency of its DSSC augments evidently. It is found that the incorporation of bis-carboxyl groups instead of the single carboxyl group as anchoring groups induces a remarkable enhancement of the electron injection efficiency from the excited dyes to the TiO2 semiconductor and generates higher electron density and voltage. Copyright
- Jia, Yongjian,Gou, Faliang,Fang, Ran,Jing, Huanwang,Zhu, Zhenping
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p. 513 - 520
(2014/07/08)
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- Detection and Imaging of Nitric Oxide with Novel Fluorescent Indicators: Diaminofluoresceins
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Nitric oxide is a gaseous, free radical which plays a role as an intracellular second messenger and a diffusable intercellular messenger. To obtain direct evidence for NO functions in vivo, we have designed and synthesized diaminofluoresceins (DAFs) as no
- Kojima, Hirotatsu,Nakatsubo, Naoki,Kikuchi, Kazuya,Kawahara, Shigenori,Kirino, Yutaka,Nagoshi, Hiroshi,Hirata, Yasunobu,Nagano, Tetsuo
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p. 2446 - 2453
(2007/10/03)
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- Development of a fluorescent indicator for nitric oxide based on the fluorescein chromophore
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Endogenous nitric oxide (NO) appears to modulate many physiological and pathophysiological processes. In order to obtain direct evidence for NO functions in vivo, we have developed 4,5-diaminofluorescein (DAF-2) as a novel fluorescent indicator for NO. Gr
- Kojima, Hirotatsu,Sakurai, Kuniko,Kikuchi, Kazuya,Kawahara, Shigenori,Kirino, Yutaka,Nagoshi, Hiroshi,Hirata, Yasunobu,Nagano, Tetsuo
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p. 373 - 375
(2007/10/03)
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- Improved synthesis of thromboxane A2 receptor antagonists with a dibenzoxepin ring system
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Two derivatives of sodium (E)-11-[2-(1-benzimidazolyl)ethylidene]11-oxo-6,11-dihydrodibenz[b,e]o xepin-2-carboxylate, novel nonprostanoid thromboxane A2 (TXA2) receptor antagonists, were synthesized from methyl 11-oxo-6,11-dihydrodibenz[b,e]oxepin-2-carboxylate. The carbonyl group at C11 was converted into a formylmethylene, then into a 1-azadiene moiety by reaction with a 2-aminoformanilide derivative. Stereo- and regioselective elaboration of the unsymmetrical imidazoles was achieved through a sequence of the transformation of E,Z-1-azadiene intermediates to E isomers under acidic conditions followed by cyclization to imidazoles.
- Sugaya,Kato,Sakaguchi,Tomioka
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p. 1257 - 1262
(2007/10/02)
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- Hypoxia-Selective Agents Derived from Quinoxaline 1,4-Di-N-oxides
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Hypoxic cells, which are a common feature of solid tumors, but not normal tissues, are resistant to both anticancer drugs and radiation therapy.Thus the identification of drugs with selective toxicity toward hypoxic cells is an important objective in anticancer chemotherapy.The benzotriazine di-N-oxide (SR 4233, Tirapazamine) has been shown to be an efficient and selective cytotoxin for hypoxic cells.Since the bioreductive activation of Tirapazamine is thought to be due to the presence of the 1,4-di-N-oxide moiety, a series of 3-aminoquinoxaline-2-carbonitrile 1,4-di-N-oxides with a range of electron-donating and -withdrawing substituents in the 6- and /or 7- positions has been synthesized and evaluated for toxicity to hypoxic cells.Electrochemical studies of the quinoxaline di-N-oxides and Tirapazamine showed that as the electron-withdrawing nature of the 6(7)-substituent increases, the reduction potential becomes more positive and the compound is more readily reduced.Apart from the unsubstituted 6a and the 6,7-dimethyl derivative 6c, the quinoxaline di-N-oxide have reduction potentials significantly more positive than Tirapazamine (Epc -0.90 V).The most potent cytotoxins to cells in culture were the 6,7-dichloro and 6,7-difluoro derivatives 6i and 6l, which were 30-fold more potent than Tirapazamine.The 6(7)-fluoro and 6(7)-chloro compounds, 6e and 6h, showed the greatest hypoxia selectivity.Four of the compounds, 6e, 6f, 6h and 6i, killed the inner cells of multicellular tumor spheroids in vitro.In vivo Balb/c mice tolerated a dose of these four compounds twice the size of that of Tirapazamine.This study demonstrates that quinoxaline 1,4-di-N-oxides could provide useful hypoxia-selective therapeutic agents.
- Monge, Antonio,Palop, Juan A.,Cerain, Adela Lopez de,Senador, Virginia,Martinez-Crespo, Francisko J.,et al.
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p. 1786 - 1792
(2007/10/02)
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