- Synthesis and photophysical properties of isocoumarin-based D-π-A systems
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We prepared a small library of polarity-sensitive fluorescent dyes characterized by an isocoumarin core properly functionalized with a conjugated push-pull system. The key step of the synthesis is based on a regio-selective silver(I)/p-TSA co-catalyzed cyclization of 2-alkynylbenzoates recently optimized in our laboratory. The photophysical properties of isocoumarin-based D-π-A systems have been investigated and a rationale was proposed based on their dipole moments and Hammett constants of the ED and EW groups involved.
- Pirovano, Valentina,Marchetti, Marialaura,Carbonaro, Jessica,Brambilla, Elisa,Rossi, Elisabetta,Ronda, Luca,Abbiati, Giorgio
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- 4,4-DIFLUORO-PIPERIDINE-COMPOUNDS
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The invention, in a first aspect relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R is a 6-membered aromatic ring, or a 5- or 6-membered heteroaromatic ring comprising 1 to 3 heteroatoms selected from S, O and N,
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Paragraph 0254; 0255; 0256; 0257
(2015/02/25)
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- Supramolecular control of selectivity in hydroformylation of vinyl arenes: Easy access to valuable β-aldehyde intermediates
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Go against the flow! A rationally designed regioselective hydroformylation catalyst, [Rh/L], in which noncovalent ligand-substrate interactions allow the unprecedented reversal of selectivity from the typical α-aldehyde to the otherwise unfavored product β-aldehyde, is reported. This catalytic system opens up novel and sustainable synthetic pathways to important intermediates for the fine-chemicals industry.
- Dydio, Pawel,Reek, Joost N. H.
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supporting information
p. 3878 - 3882
(2013/05/09)
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- 4,4-DIFLUORO-PIPERIDINE-COMPOUNDS
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The invention, in a first aspect relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R is a 6-membered aromatic ring, or a 5- or 6-membered heteroaromatic ring comprising 1 to 3 heteroatoms selected from S, O and N,
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Page/Page column 21
(2013/09/12)
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- Monna, a potent and selective blocker for transmembrane protein with unknown function 16/anoctamin-1
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Transmembrane protein with unknown function 16/anoctamin-1 (ANO1) is a protein widely expressed in mammalian tissues, and it has the properties of the classic calcium-activated chloride channel (CaCC). This protein has been implicated in numerous major physiological functions. However, the lack of effective and selective blockers has hindered a detailed study of the physiological functions of this channel. In this study, we have developed a potent and selective blocker for endogenous ANO1 in Xenopus laevis oocytes (xANO1) using a drug screening method we previously established (Oh et al., 2008). We have synthesized a number of anthranilic acid derivatives and have determined the correlation between biological activity and the nature and position of substituents in these derived compounds. A structure-activity relationship revealed novel chemical classes of xANO1 blockers. The derivatives contain a-NO2 group on position 5 of a naphthyl group-substituted anthranilic acid, and they fully blocked xANO1 chloride currents with an IC 5050 of 0.08 μM for xANO1. Selectivity tests revealed that other chloride channels such as bestrophin-1, chloride channel protein 2, and cystic fibrosis transmembrane conductance regulator were not appreciably blocked by 10~30 μM MONNA. The potent and selective blockers for ANO1 identified here should permit pharmacological dissection of ANO1/CaCC function and serve as potential candidates for drug therapy of related diseases such as hypertension, cystic fibrosis, bronchitis, asthma, and hyperalgesia.
- Oh, Soo-Jin,Hwang, Seok Jin,Jung, Jonghoon,Yu, Kuai,Kim, Jeongyeon,Choi, Jung Yoon,Hartzell, H. Criss,Roh, Eun Joo,Justin Lee
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p. 726 - 735
(2013/11/06)
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- Donor-acceptor biaryl lactones: PH induced molecular switches with intramolecular charge transfer modulation
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The physical properties of biaryl-containing compounds are known to be highly dependent on molecular geometry. We report the syntheses and fundamental spectroscopic study of two donor-acceptor biaryl lactone (6H-benzo[c]chromen-6- one) pH-driven switches.
- Carlson, Erik J.,Riel, Asia Marie S.,Dahl, Bart J.
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supporting information
p. 6245 - 6249,5
(2012/12/11)
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- NOVEL ANTHRANILIC ACID DERIVATIVES AND CHLORIDE CHANNEL BLOCKING AGENT CONTAINING THE SAME
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The present invention relates to novel anthranilic acid derivatives represented by Chemical Formula I, and a chloride channel blocking agent containing the anthranilic acid derivative or its pharmacologically acceptable salts as an active ingredient. In another aspect, the present invention relates to a method of accurately and efficiently detecting the intracellular chloride channel inhibition and method of screening a chloride channel blocking agent.
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Page/Page column 8
(2009/05/28)
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- Water-soluble polyimides and methods of making and using same
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The present invention provides, among other things, water-soluble polyimides, methods of making water-soluble polyimides, and methods of using water-soluble polyimides, e.g., in optics applications as well as other applications.
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Page/Page column 15
(2008/06/13)
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- Regiospecific synthesis of substituted nitrofluorenes and aminofluorenes with the Negishi coupling reaction as key step
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A short regiospecific route to 7-alkyl/CF3 substituted 2-nitrofluorenes and 2-aminofluorenes is described. The synthesis takes advantage of the palladium(0)-catalysed Negishi coupling of methyl 2-bromo-5-nitrobenzoate with aromatic zinc species
- Klein,Boche
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p. 1246 - 1250
(2007/10/03)
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