- IMPROVER FOR INFLAMMATORY DISEASE OR ISCHEMIC DISEASE
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PROBLEM TO BE SOLVED: To provide a new improver for inflammatory disease or ischemic disease. SOLUTION: The present invention provides an improver for inflammatory disease or acute ischemic disease containing an MAIT cell function inhibitor as an active ingredient. SELECTED DRAWING: None COPYRIGHT: (C)2019,JPOandINPIT
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Paragraph 0042; 0043; 0044
(2019/07/20)
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- Folic acid-conjugated europium complexes as luminescent probes for selective targeting of cancer cells
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We report the synthesis of three optical probes (Eu3+1, Eu3+2, and Eu3+3) having a luminescent Eu complex (signaling unit) bonded in different positions to folic acid (FA), the folate receptor (FR) targeting unit. The structures of the two regioisomers Eu3+1 and Eu3+2 were assigned by mass spectrometric experiments. The optical properties and stability of these probes were assessed in phosphate-buffered saline, cell culture medium, rat serum, and cellular lysate, and results indicated that they are chemically and photophysically stable. Cytotoxicity was studied with ovarian cancer cells having high (SKOV-3), intermediate (OVCAR-3), low (IGROV-1), or null (A2780) expression of FRs. The internalized probe, evaluated in SKOV-3, IGROV-1, and A2780 cells, was in the order Eu3+2 > Eu3+1 > Eu3+3. No internalization was observed for A2780 cells. Such results, together with those obtained in competition experiments of FA versus Eu3+2 and FA or Eu3+2 versus 3H-FA, indicate that internalization is receptor-mediated and that Eu3+2 shows high selectivity and specificity for FR.
- Quici, Silvio,Casoni, Alessandro,Foschi, Francesca,Armelao, Lidia,Bottaro, Gregorio,Seraglia, Roberta,Bolzati, Cristina,Salvarese, Nicola,Carpanese, Debora,Rosato, Antonio
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supporting information
p. 2003 - 2014
(2015/04/27)
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- Reaction between 7,8-dihydropterins and hydrogen peroxide under physiological conditions
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In vitiligo, a common skin disorder that produces white patches of depigmentation, 7,8-dihydropterins accumulate in the presence of high concentration of H2O2. In this work, we present a study of the reaction between 7,8-dihydropterins and H2O2. The rate of the reaction, as well as the products formed, strongly depend on the chemical structure of the substituents. Electron-donor groups as substituents are the most reactive derivatives and undergo oxidation of the pterin moiety. The corresponding bimolecular rate constants at 37 °C in neutral aqueous solutions are reported. The biological implications of the results obtained are also discussed.
- Laura Dántola,Schuler, Tobias M.,Paula Denofrio,Vignoni, Mariana,Capparelli, Alberto L.,Lorente, Carolina,Thomas, Andrés H.
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p. 8692 - 8699
(2008/12/21)
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- Stability of 7,8-dihydropterins in air-equilibrated aqueous solutions
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6-Substituted 7,8-dihydropterins (=2-amino-7,8-dihydropteridin-4(1H)-ones) are heterocyclic compounds that occur in a wide range of living systems and participate in relevant biological functions. In airequilibrated aqueous solutions, these compounds react with dissolved O2 (autooxidation). The rates of these reactions as well as the products formed strongly depend on the chemical structure of the substituents. 7,8-Dihydro-6-methylpterin and 7,8-dihydro-6,7-dimethylpterin that bear electron-donor groups as substituents are the most reactive derivatives and undergo oxidation of the pterin moiety to yield the corresponding oxidized derivatives (6-methylpterin and 6,7-dimethylpterin, resp.). The oxidations of 7,8-dihydrobiopterin, 7,8-dihydroneopterin, and 7,8-dihydrofolic acid are slower, and they yield 7,8-dihydroxanthopterin as the main product. 7,8-Dihydroxanthopterin, 6-formyl-7,8-dihydropterin, and sepiapterin are rather stable, and their consumption in air-equilibrated solutions is negligible for several days. The pseudo-first-order rate constants of the reactions between these compounds and O2 at 25° and 40° are reported. The biological implications of the results obtained are also discussed.
- Dantola, M. Laura,Vignoni, Mariana,Capparelli, Alberto L.,Lorente, Carolina,Thomas, Andres H.
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body text
p. 411 - 425
(2009/02/07)
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- One-step synthesis of lumazine and xanthine: First co-crystal of lumazine and perchloric acid with a unique monohydrated hydronium ion (H 5O2+) mediated supramolecular assembly of the lumazine dimer
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A perchloric acid mediated one-step synthesis of lumazine derivatives from pterins and xanthine from guanine is reported. However, 2-pivaloylamino derivatives of pterins underwent simple hydrolysis of the pivaloylamino group generating free pterin compounds, but the 2-oxo derivatives, that is, the lumazine compounds, were not obtained. A novel supramolecular assembly is constructed by the unique hydrogen bonding of H5O2 + bridging two hydrogen-bonded dimers of lumazine to form the co-crystal 21 with aqueous perchloric acid. In contrast, N2-pivaloyl- 6-bromo-5-deazapterin was simply hydrolysed to form the protonated deazapterin 22, which forms a unique six-membered cyclic hydrogen-bonded structure leading to the generation of a polymeric supramolecular assembly. Wiley-VCH Verlag GmbH & Co. KGaA, 2007.
- Goswami, Shyamaprosad,Maity, Annada C.,Fun, Hoong-Kun
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p. 4056 - 4064
(2008/02/13)
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- The first microwave-assisted regiospecific synthesis of 6-substituted pterins
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The pyrazine ring was developed in a pyrimidine and in a benzene by Isay type condensations under microwave irradiation to afford pterin and quinoxaline systems. Interestingly, the desired isomerically free 6-substituted pterins including pterin sugar derivatives were synthesised in moderate to good yields whereas mixtures of both 6- and 7-isomers (major) are generally obtained using conventional Isay type condensations.
- Goswami, Shyamaprosad,Adak, Avijit Kumar
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p. 8371 - 8373
(2007/10/03)
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- RING TRANSFORMATION OF PTERINS TO GUANINES
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7-Alkoxypterins undergo a ring contraction into guanine derivatives and demethoxylation by activated aluminum.
- Sugimoto, Takashi,Nishioka, Noriko,Murata, Shizuaki,Matsuura, Sadao
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p. 2091 - 2092
(2007/10/02)
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- SYNTHESIS OF QUINONOID 6-METHYL AND 6,7-DIMETHYLDIHYDROPTERINS
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Quinonoid 6-methyl and 6,7-dimethylpterins were synthesized by the chemical oxidation.Some of their properties are described.
- Matsuura, Sadao,Sugimoto, Takashi,Murata, Shizuaki
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p. 4003 - 4004
(2007/10/02)
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- Pterins. X A New Preparation of 6-Hydroxymethylpterin from 6-Methylpterin
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6-Hydroxymethylpterin was prepared in c. 80percent overall yield via 2-acetamido-6-methylpteridin-4(3H)-one, oxidation with lead tetraacetate to 2-acetamido-6-acetoxymethylpteridin-4(3H)-one and hydrolysis.The 2-acetamido-6-methylpterin was prepared isomerically pure by acetylation of a mixture of 6- and 7-methylpterin prepared by condensation of 2,5,6-triaminopyrimidin-4(3H)-one with methylglyoxal at 0-5 deg.Under these conditions the ratio of 6-methyl to 7-methylpterin is considerably improved (9:1).
- Waring, Paul,Armarego, Wilfred, L. F.
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p. 629 - 631
(2007/10/02)
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- 185. Ueber Pterinchemie. Zum Verlauf der katalytischen Reduktion von 6-Methylpterin
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The catalytic hydrogenation of 6-methylpterin (I) in neutral or weekly acidic solutions begins, as for the 7-methylpterin, by the thermodynamically controlled reduction of the 7,8-double bond.It is not possible to say, according to our experiments, which double bond, either the 5,6 or the 7,8, is first reduced in strongly acidic solution.However, a 5,8-reduction can be excluded.
- Ganguly, Abhoy N.,Sengupta, Pradip K.,Bieri, Jost H.,Visconti, Max
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p. 1754 - 1758
(2007/10/02)
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