- XANTHENE COMPOUND, COLORING COMPOSITION CONTAINING THE COMPOUND, COLORANT FOR COLOR FILTERS AND COLOR FILTER
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PROBLEM TO BE SOLVED: To provide a xanthene compound, a coloring composition containing the compound, a colorant for color filters containing the coloring composition, and a color filter including the colorant. SOLUTION: A xanthene compound represented by
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Paragraph 0087-0089
(2020/08/25)
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- Deciphering the Mechanism of Human Carbonic Anhydrases Inhibition with Sulfocoumarins: Computational and Experimental Studies
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The reaction mechanism of the carbonic anhydrase-mediated hydrolysis of sulfocoumarins to sulfonic acids has been investigated on an enzyme cluster model using the B3LYP hybrid density functional theory (DFT) and the QST procedure for the Transition State (TS) search. A multistep process was highlighted, with the rate-determining step identified in the initial dual nucleophilic/acidic attack of the zinc-bound hydroxide ion to the sulfocoumarin sulfur atom and to the C3=C4 double bond. The reported multi-step process, combined to SAR analysis on a new set of derivatives, highlighted unprecedented mechanistic aspects of the CA-mediated prodrug activation, which in turn possess relevant consequences to the isoforms-selective inhibition profiles reported by such a class of compounds.
- Nocentini, Alessio,Carta, Fabrizio,Tanc, Muhammet,Selleri, Silvia,Supuran, Claudiu T.,Bazzicalupi, Carla,Gratteri, Paola
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supporting information
p. 7840 - 7844
(2018/05/08)
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- Thiazole amide compound and preparation method, pharmaceutical composition and application thereof
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The invention discloses a thiazole amide compound and a preparation method thereof, a pharmaceutical composition and application thereof. The thiazole amide compound as shown in a formula I and a pharmaceutically acceptable salt thereof are provided, and
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Paragraph 0207; 0231; 0269; 0270; 0271
(2019/01/08)
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- Glyoxalase 1 and 2 enzyme inhibitory activity of 6-sulfamoylsaccharin and sulfocoumarin derivates
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The glyoxalase enzymes represent a cellular defence system against the accumulation of cytotoxic α-oxoaldehydes leading to apoptosis. The potential of glyoxalase inhibitors to act as novel anti-cancer agents for drugresistant tumours that over-express gly
- Makrecka, Marina,Zalubovskis, Raivis,Vavers, Edijs,Ivanova, Jekaterina,Grandane, Aiga,Dambrova, Maija
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p. 410 - 414
(2013/07/26)
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- Facile synthesis of coumarin bioisosteres - 1,2-benzoxathiine 2,2-dioxides
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A simple and reproducible procedure for the synthesis of bioisosteres of coumarin - 1,2-benzoxathiine 2,2-dioxide is presented. The developed method is based on the intramolecular aldol cyclization of derivatives of mesylsalicyl aldehydes in the presence
- Grandane, Aiga,Belyakov, Sergey,Trapencieris, Peteris,Zalubovskis, Raivis
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experimental part
p. 5541 - 5546
(2012/09/07)
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- NOVEL CURCUMIN DERIVATIVE
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To develop a highly safe measure to treat Alzheimer's disease using a secretase-inhibiting substance, there is provided a compound represented by the following general formula (I) or a salt thereof: wherein A represents a phenyl group or the like, R1 represents a chlorine atom, a bromine atom, or a nitro group or the like, R2, R3, R4, and R5 each represent a hydrogen atom or the like, and L represents CH2—CH2 or CH═CH.
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Page/Page column 23
(2011/04/24)
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- NOVEL CURCUMIN DERIVATIVE
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The present invention provides a novel compound that is structurally similar to curcumin and has a suppressive effect on Aβ aggregation, a degradative effect on Aβ aggregates, an inhibitory effect on β-secretase, and a protective effect on neurons. The novel compound is a compound represented by the following general formula (Ia) or a salt thereof: wherein R1 represents a 4-hydroxy-3-methoxyphenyl group or the like, and R2 represents a 1H-indol-6-yl group or the like.
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Page/Page column 96
(2009/12/07)
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