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Josephine Spitzer - One of the best experts on this subject based on the ideXlab platform.
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Discovery of a novel series of 6-Azauracil-based thyroid hormone receptor ligands: Potent, TRβ subtype-selective thyromimetics
Bioorganic & medicinal chemistry letters, 2003Co-Authors: Robert L. Dow, Steven R. Schneider, Ernest S. Paight, Richard F. Hank, Phoebe Chiang, Peter Cornelius, Eunsun Lee, William P. Newsome, Andrew G. Swick, Josephine SpitzerAbstract:Abstract In this communication, we wish to describe the discovery of a novel series of 6-Azauracil-based thyromimetics that possess up to 100-fold selectivities for binding and functional activation of the β1-isoform of the thyroid receptor family. Structure–activity relationship studies on the 3,5- and 3′-positions provided compounds with enhanced TRβ affinity and selectivity. Key binding interactions between the 6-Azauracil moiety and the receptor have been determined through of X-ray crystallographic analysis.
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Discovery of a novel series of 6-Azauracil-based thyroid hormone receptor ligands: Potent, TRβ subtype-selective thyromimetics
Bioorganic & medicinal chemistry letters, 2003Co-Authors: Robert L. Dow, Steven R. Schneider, Ernest S. Paight, Richard F. Hank, Phoebe Chiang, Peter Cornelius, Eunsun Lee, William P. Newsome, Swick Andrew Gordon, Josephine SpitzerAbstract:In this communication, we wish to describe the discovery of a novel series of 6-Azauracil-based thyromimetics that possess up to 100-fold selectivities for binding and functional activation of the beta(1)-isoform of the thyroid receptor family. Structure-activity relationship studies on the 3,5- and 3'-positions provided compounds with enhanced TR beta affinity and selectivity. Key binding interactions between the 6-Azauracil moiety and the receptor have been determined through of X-ray crystallographic analysis.
Jan Slouka - One of the best experts on this subject based on the ideXlab platform.
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Synthesis of some symmetrically substituted compounds derived from 1,3-bis(6-Azauracil-1-yl)benzene and 1,3,5-tris(6-Azauracil-1-yl)benzene
Journal of Heterocyclic Chemistry, 2002Co-Authors: Petr Bilek, Jan SloukaAbstract:The 3,5-bis(5-carboxy-6-Azauracil-1-yl)aniline (7) and 1,3,5-tris(5-carboxy-6-Azauracil-1-yl)benzene (10) were prepared from 3-amino-5-nitroacetanilide (1) via intermediates 2–6. A series of other substituted 6-Azauracil derivatives 9, 11-14 were also prepared.
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1-ARYL-6-AzauracilS XLI # SYNTHESIS AND REACTIVITY OF 1-(3,5-DINITROPHENYL) -6-Azauracil-5-CARBONITRILE
2001Co-Authors: Facultas Rerum Naturalium, Petr Bilek, Jan SloukaAbstract:Diazotization of 3,5-dinitroaniline either in acetic acid or nitrosylsulphuric acid afforded diazonium salt that after coupling either with ethyl cyanoacetylcarbamate or diethyl malonylbiscarbamate afforded corresponding hydrazones (2a) or (2b) respectively. After cyclization of (2a) in xylene we received 3,5-dinitrophenyl-6-Azauracil derivative (3a). This derivative underwent hydrolytic splitting of the triazine cycle by boiling in water pyridine solution resulting in 3,5-dinitrophenylhydrazonocyanoacetamide (4a) that was impossible to obtain directly by coupling reaction.
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1-ARYL-6-AzauracilS XLI # SYNTHESIS AND REACTIVITY OF 1-(3,5-DINITROPHENYL)-6-Azauracil-5-CARBONITRILE
2001Co-Authors: Facultas Rerum, Naturalium Chemica, Petr Bilek, Jan SloukaAbstract:Diazotization of 3,5-dinitroaniline either in acetic acid or nitrosylsulphuric acid afforded diazonium salt that after coupling either with ethyl cyanoacetylcarbamate or diethyl malonylbiscarbamate afforded corresponding hydrazones (2a) or (2b) respectively. After cyclization of (2a) in xylene we received 3,5-dinitrophenyl-6-Azauracil derivative (3a). This derivative underwent hydrolytic splitting of the triazine cycle by boiling in water pyridine solution resulting in 3,5-dinitrophenylhydrazonocyanoacetamide (4a) that was impossible to obtain directly by coupling reaction. Key words: Coupling reactions of 3,5-dinitrobenzenediazonium salts, splittin
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SYNTHESIS OF 5-(M-TOLYL)-6-Azauracil AND SOME OF ITS DERIVATIVES
2000Co-Authors: Facultas Rerum, Naturalium Chemica, Jan Hlaváč, Jan Slouka, Pavel Hradil, Ar NAbstract:7-Methylisatin (I) was converted to appropriate semicarbazone (II). Its alkaline recyclization afforded 5-(2-amino-3-methyl)-6-Azauracil (III). Its diazotation and subsequent reductive elimination of diazonium group led to the 5-(m-tolyl)-6-Azauracil (VI). Appropriate hydrazone (V) was prepared by coupling of diazotated amine III with ethyl cyanoacetylcarbamate. After reaction with bicarbonate this compound was converted to 1-[2-(6-Azauracil-5-yl)-6-methylphenyl]-6-Azauracil-5-carbonitrile (VII). Cyclization of aminoderivative III afforded 3,5-dihydro-5H-6-methyl-[1,2,4]triazino[5,6-b]indole-3-one (VII) Key words: 5-aryl-6-Azauracils, twocyclic 6-Azauracils, [1,2,4]-triazino[5,6-b]indol
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1-ARYL-6-AzauracilS XL* SYNTHESIS OF SOME 1-(1-PHENYL-3-PYRAZOLYL)- DERIVATIVES
2000Co-Authors: Facultas Rerum, Naturalium Chemica, Petr Cankař, Jan SloukaAbstract:The appropriate hydrazone I was obtained by the diazotation of 1-phenyl-3aminopyrazole and by the following coupling reaction of formed diazonium salt with ethyl cyanoacetyl carbamate. The cyclization of this hydrazone does not undergo to the appropriate derivative pyrazolo[5,1-c][1,2,4]triazine, but both the thermal and the alkaline cyclization undergoes to 1-(1-phenyl-3-pyrazolyl)-6-Azauracil-5-carbonitrile II. This compound serves as a starting material for the appropriate acid III, amidoxime IV and 1-(1-phenyl-3-pyrazolyl)-5-(5-methyl-[1,2,4]oxadiazol-3-yl)-6Azauracile V. Key words: 1,2,4-triazine, 1,5-disubstituted 6-Azauracils, 1,3-disubstituted pyrazole
Robert L. Dow - One of the best experts on this subject based on the ideXlab platform.
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Discovery of a novel series of 6-Azauracil-based thyroid hormone receptor ligands: Potent, TRβ subtype-selective thyromimetics
Bioorganic & medicinal chemistry letters, 2003Co-Authors: Robert L. Dow, Steven R. Schneider, Ernest S. Paight, Richard F. Hank, Phoebe Chiang, Peter Cornelius, Eunsun Lee, William P. Newsome, Andrew G. Swick, Josephine SpitzerAbstract:Abstract In this communication, we wish to describe the discovery of a novel series of 6-Azauracil-based thyromimetics that possess up to 100-fold selectivities for binding and functional activation of the β1-isoform of the thyroid receptor family. Structure–activity relationship studies on the 3,5- and 3′-positions provided compounds with enhanced TRβ affinity and selectivity. Key binding interactions between the 6-Azauracil moiety and the receptor have been determined through of X-ray crystallographic analysis.
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Discovery of a novel series of 6-Azauracil-based thyroid hormone receptor ligands: Potent, TRβ subtype-selective thyromimetics
Bioorganic & medicinal chemistry letters, 2003Co-Authors: Robert L. Dow, Steven R. Schneider, Ernest S. Paight, Richard F. Hank, Phoebe Chiang, Peter Cornelius, Eunsun Lee, William P. Newsome, Swick Andrew Gordon, Josephine SpitzerAbstract:In this communication, we wish to describe the discovery of a novel series of 6-Azauracil-based thyromimetics that possess up to 100-fold selectivities for binding and functional activation of the beta(1)-isoform of the thyroid receptor family. Structure-activity relationship studies on the 3,5- and 3'-positions provided compounds with enhanced TR beta affinity and selectivity. Key binding interactions between the 6-Azauracil moiety and the receptor have been determined through of X-ray crystallographic analysis.
Peter Cornelius - One of the best experts on this subject based on the ideXlab platform.
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Discovery of a novel series of 6-Azauracil-based thyroid hormone receptor ligands: Potent, TRβ subtype-selective thyromimetics
Bioorganic & medicinal chemistry letters, 2003Co-Authors: Robert L. Dow, Steven R. Schneider, Ernest S. Paight, Richard F. Hank, Phoebe Chiang, Peter Cornelius, Eunsun Lee, William P. Newsome, Andrew G. Swick, Josephine SpitzerAbstract:Abstract In this communication, we wish to describe the discovery of a novel series of 6-Azauracil-based thyromimetics that possess up to 100-fold selectivities for binding and functional activation of the β1-isoform of the thyroid receptor family. Structure–activity relationship studies on the 3,5- and 3′-positions provided compounds with enhanced TRβ affinity and selectivity. Key binding interactions between the 6-Azauracil moiety and the receptor have been determined through of X-ray crystallographic analysis.
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Discovery of a novel series of 6-Azauracil-based thyroid hormone receptor ligands: Potent, TRβ subtype-selective thyromimetics
Bioorganic & medicinal chemistry letters, 2003Co-Authors: Robert L. Dow, Steven R. Schneider, Ernest S. Paight, Richard F. Hank, Phoebe Chiang, Peter Cornelius, Eunsun Lee, William P. Newsome, Swick Andrew Gordon, Josephine SpitzerAbstract:In this communication, we wish to describe the discovery of a novel series of 6-Azauracil-based thyromimetics that possess up to 100-fold selectivities for binding and functional activation of the beta(1)-isoform of the thyroid receptor family. Structure-activity relationship studies on the 3,5- and 3'-positions provided compounds with enhanced TR beta affinity and selectivity. Key binding interactions between the 6-Azauracil moiety and the receptor have been determined through of X-ray crystallographic analysis.
Phoebe Chiang - One of the best experts on this subject based on the ideXlab platform.
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Discovery of a novel series of 6-Azauracil-based thyroid hormone receptor ligands: Potent, TRβ subtype-selective thyromimetics
Bioorganic & medicinal chemistry letters, 2003Co-Authors: Robert L. Dow, Steven R. Schneider, Ernest S. Paight, Richard F. Hank, Phoebe Chiang, Peter Cornelius, Eunsun Lee, William P. Newsome, Andrew G. Swick, Josephine SpitzerAbstract:Abstract In this communication, we wish to describe the discovery of a novel series of 6-Azauracil-based thyromimetics that possess up to 100-fold selectivities for binding and functional activation of the β1-isoform of the thyroid receptor family. Structure–activity relationship studies on the 3,5- and 3′-positions provided compounds with enhanced TRβ affinity and selectivity. Key binding interactions between the 6-Azauracil moiety and the receptor have been determined through of X-ray crystallographic analysis.
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Discovery of a novel series of 6-Azauracil-based thyroid hormone receptor ligands: Potent, TRβ subtype-selective thyromimetics
Bioorganic & medicinal chemistry letters, 2003Co-Authors: Robert L. Dow, Steven R. Schneider, Ernest S. Paight, Richard F. Hank, Phoebe Chiang, Peter Cornelius, Eunsun Lee, William P. Newsome, Swick Andrew Gordon, Josephine SpitzerAbstract:In this communication, we wish to describe the discovery of a novel series of 6-Azauracil-based thyromimetics that possess up to 100-fold selectivities for binding and functional activation of the beta(1)-isoform of the thyroid receptor family. Structure-activity relationship studies on the 3,5- and 3'-positions provided compounds with enhanced TR beta affinity and selectivity. Key binding interactions between the 6-Azauracil moiety and the receptor have been determined through of X-ray crystallographic analysis.
