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Enrique Ravina - One of the best experts on this subject based on the ideXlab platform.
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pyridazines part 36 synthesis and antiplatelet activity of 5 substituted 6 phenyl 3 2h Pyridazinones
Bioorganic & Medicinal Chemistry Letters, 2004Co-Authors: Alberto Coelho, Eddy Sotelo, Nuria Fraiz, Matilde Yanez, Reyes Laguna, Ernesto Cano, Enrique RavinaAbstract:A convenient and efficient palladium-catalysed retro-ene-assisted method has been developed to prepare a series of 5-substituted-6-phenyl-3(2H)-Pyridazinones as potential antiplatelet drugs. The most active compounds were those that contain a 3-phenyl-3-oxo-propenyl fragment or a phenylthio group at position 5 of the heterocyclic ring.
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pyridazines part xxix synthesis and platelet aggregation inhibition activity of 5 substituted 6 phenyl 3 2h Pyridazinones novel aspects of their biological actions
Bioorganic & Medicinal Chemistry, 2002Co-Authors: Eddy Sotelo, Nuria Fraiz, Matilde Yanez, Reyes Laguna, Ernesto Cano, Vicente Terrades, Enrique RavinaAbstract:A series of 6-phenyl-3(2H)-Pyridazinones with a diverse range of substituents in the 5-position have been prepared and evaluated in the search for new antiplatelet agents. A significant dependence of the substituent on the inhibitory effect has been observed. The pharmacological study of these compounds confirms that modification of the chemical group at position 5 of the 6-phenyl-3(2H)-Pyridazinone system influences both variations in the antiplatelet activity and the mechanism of action.
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pyridazines part 28 5 alkylidene 6 phenyl 3 2h Pyridazinones a new family of platelet aggregation inhibitors
Bioorganic & Medicinal Chemistry Letters, 2002Co-Authors: Eddy Sotelo, Nuria Fraiz, Matilde Yanez, Reyes Laguna, Ernesto Cano, Jose Brea, Enrique RavinaAbstract:The synthesis and anti-platelet activity of several 5-alkylidene-6-phenyl-3(2H)-Pyridazinones are described. The most active compounds are those that contain oxygenated functions (COOR, COMe) on the alkylidene fragment (6a, 6b and 6c).
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pyridazine derivatives part 21 synthesis and structural study of novel 4 aryl 2 5 dioxo 8 phenylpyrido 2 3 d pyridazines
Tetrahedron, 2000Co-Authors: Eddy Sotelo, Enrique Ravina, Beatriz Pita, Margarita Suarez, Estael Ochoa, Yamila Verdecia, Hector Novoa, Norbert Blaton, Caimle De RanterAbstract:Abstract New substituted 4-aryl-2,5-dioxo-8-phenylpyrido[2,3-d]pyridazines 4a–f have been prepared in one step from the corresponding arylidene substituted Meldrum's acid (1) and 5-amino-6-phenyl-3(2H)-Pyridazinone (2) in good yields. Semiempirical theoretical calculations (AM1) reveal two favoured conformations (A and B) for compounds 4a–f, with a screw boat conformation in the pyridone system and a planar Pyridazinone ring. X-Ray crystallographic analysis shows that in the solid state, conformation A bearing the phenyl ring in a pseudoaxial position is the most stable. Compounds 4a–f fulfil, from the structural point of view, all the requirements needed for exhibiting cardiotonic effects.
Eddy Sotelo - One of the best experts on this subject based on the ideXlab platform.
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pyridazines part 36 synthesis and antiplatelet activity of 5 substituted 6 phenyl 3 2h Pyridazinones
Bioorganic & Medicinal Chemistry Letters, 2004Co-Authors: Alberto Coelho, Eddy Sotelo, Nuria Fraiz, Matilde Yanez, Reyes Laguna, Ernesto Cano, Enrique RavinaAbstract:A convenient and efficient palladium-catalysed retro-ene-assisted method has been developed to prepare a series of 5-substituted-6-phenyl-3(2H)-Pyridazinones as potential antiplatelet drugs. The most active compounds were those that contain a 3-phenyl-3-oxo-propenyl fragment or a phenylthio group at position 5 of the heterocyclic ring.
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pyridazines part xxix synthesis and platelet aggregation inhibition activity of 5 substituted 6 phenyl 3 2h Pyridazinones novel aspects of their biological actions
Bioorganic & Medicinal Chemistry, 2002Co-Authors: Eddy Sotelo, Nuria Fraiz, Matilde Yanez, Reyes Laguna, Ernesto Cano, Vicente Terrades, Enrique RavinaAbstract:A series of 6-phenyl-3(2H)-Pyridazinones with a diverse range of substituents in the 5-position have been prepared and evaluated in the search for new antiplatelet agents. A significant dependence of the substituent on the inhibitory effect has been observed. The pharmacological study of these compounds confirms that modification of the chemical group at position 5 of the 6-phenyl-3(2H)-Pyridazinone system influences both variations in the antiplatelet activity and the mechanism of action.
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pyridazines part 28 5 alkylidene 6 phenyl 3 2h Pyridazinones a new family of platelet aggregation inhibitors
Bioorganic & Medicinal Chemistry Letters, 2002Co-Authors: Eddy Sotelo, Nuria Fraiz, Matilde Yanez, Reyes Laguna, Ernesto Cano, Jose Brea, Enrique RavinaAbstract:The synthesis and anti-platelet activity of several 5-alkylidene-6-phenyl-3(2H)-Pyridazinones are described. The most active compounds are those that contain oxygenated functions (COOR, COMe) on the alkylidene fragment (6a, 6b and 6c).
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pyridazine derivatives part 21 synthesis and structural study of novel 4 aryl 2 5 dioxo 8 phenylpyrido 2 3 d pyridazines
Tetrahedron, 2000Co-Authors: Eddy Sotelo, Enrique Ravina, Beatriz Pita, Margarita Suarez, Estael Ochoa, Yamila Verdecia, Hector Novoa, Norbert Blaton, Caimle De RanterAbstract:Abstract New substituted 4-aryl-2,5-dioxo-8-phenylpyrido[2,3-d]pyridazines 4a–f have been prepared in one step from the corresponding arylidene substituted Meldrum's acid (1) and 5-amino-6-phenyl-3(2H)-Pyridazinone (2) in good yields. Semiempirical theoretical calculations (AM1) reveal two favoured conformations (A and B) for compounds 4a–f, with a screw boat conformation in the pyridone system and a planar Pyridazinone ring. X-Ray crystallographic analysis shows that in the solid state, conformation A bearing the phenyl ring in a pseudoaxial position is the most stable. Compounds 4a–f fulfil, from the structural point of view, all the requirements needed for exhibiting cardiotonic effects.
Matilde Yanez - One of the best experts on this subject based on the ideXlab platform.
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new Pyridazinone derivatives with vasorelaxant and platelet antiaggregatory activities
ChemInform, 2011Co-Authors: Tamara Costas, Matilde Yanez, Reyes Laguna, Pedro Besada, Alessandro Piras, Laura Acevedo, Francisco Orallo, Carmen TeranAbstract:Novel Pyridazinones (III), (VI), (VIIb), (IXa), and (XIb) demonstrate moderate vasorelaxant activity and moderate to potent inhibition of collagen-induced platelet aggregation.
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new Pyridazinone derivatives with vasorelaxant and platelet antiaggregatory activities
Bioorganic & Medicinal Chemistry Letters, 2010Co-Authors: Tamara Costas, Matilde Yanez, Reyes Laguna, Pedro Besada, Alessandro Piras, Laura Acevedo, Francisco Orallo, Carmen TeranAbstract:New 6-substituted and 2,6-disubstituted Pyridazinone derivatives were obtained starting from easily accessible alkyl furans by using oxidation with singlet oxygen to give 4-methoxy or 4-hydroxybutenolides, key intermediates of this synthetic strategy. The new Pyridazinone derivatives have been studied as vasorelaxant and antiplatelet agents. Analysis of biological data revealed the silyl ethers (4a-i) and N,O-dibenzyl derivatives (6g-i) as the most active compounds. © 2010 Elsevier Ltd. All rights reserved.
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pyridazines part 36 synthesis and antiplatelet activity of 5 substituted 6 phenyl 3 2h Pyridazinones
Bioorganic & Medicinal Chemistry Letters, 2004Co-Authors: Alberto Coelho, Eddy Sotelo, Nuria Fraiz, Matilde Yanez, Reyes Laguna, Ernesto Cano, Enrique RavinaAbstract:A convenient and efficient palladium-catalysed retro-ene-assisted method has been developed to prepare a series of 5-substituted-6-phenyl-3(2H)-Pyridazinones as potential antiplatelet drugs. The most active compounds were those that contain a 3-phenyl-3-oxo-propenyl fragment or a phenylthio group at position 5 of the heterocyclic ring.
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pyridazines part xxix synthesis and platelet aggregation inhibition activity of 5 substituted 6 phenyl 3 2h Pyridazinones novel aspects of their biological actions
Bioorganic & Medicinal Chemistry, 2002Co-Authors: Eddy Sotelo, Nuria Fraiz, Matilde Yanez, Reyes Laguna, Ernesto Cano, Vicente Terrades, Enrique RavinaAbstract:A series of 6-phenyl-3(2H)-Pyridazinones with a diverse range of substituents in the 5-position have been prepared and evaluated in the search for new antiplatelet agents. A significant dependence of the substituent on the inhibitory effect has been observed. The pharmacological study of these compounds confirms that modification of the chemical group at position 5 of the 6-phenyl-3(2H)-Pyridazinone system influences both variations in the antiplatelet activity and the mechanism of action.
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pyridazines part 28 5 alkylidene 6 phenyl 3 2h Pyridazinones a new family of platelet aggregation inhibitors
Bioorganic & Medicinal Chemistry Letters, 2002Co-Authors: Eddy Sotelo, Nuria Fraiz, Matilde Yanez, Reyes Laguna, Ernesto Cano, Jose Brea, Enrique RavinaAbstract:The synthesis and anti-platelet activity of several 5-alkylidene-6-phenyl-3(2H)-Pyridazinones are described. The most active compounds are those that contain oxygenated functions (COOR, COMe) on the alkylidene fragment (6a, 6b and 6c).
Reyes Laguna - One of the best experts on this subject based on the ideXlab platform.
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new Pyridazinone derivatives with vasorelaxant and platelet antiaggregatory activities
ChemInform, 2011Co-Authors: Tamara Costas, Matilde Yanez, Reyes Laguna, Pedro Besada, Alessandro Piras, Laura Acevedo, Francisco Orallo, Carmen TeranAbstract:Novel Pyridazinones (III), (VI), (VIIb), (IXa), and (XIb) demonstrate moderate vasorelaxant activity and moderate to potent inhibition of collagen-induced platelet aggregation.
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new Pyridazinone derivatives with vasorelaxant and platelet antiaggregatory activities
Bioorganic & Medicinal Chemistry Letters, 2010Co-Authors: Tamara Costas, Matilde Yanez, Reyes Laguna, Pedro Besada, Alessandro Piras, Laura Acevedo, Francisco Orallo, Carmen TeranAbstract:New 6-substituted and 2,6-disubstituted Pyridazinone derivatives were obtained starting from easily accessible alkyl furans by using oxidation with singlet oxygen to give 4-methoxy or 4-hydroxybutenolides, key intermediates of this synthetic strategy. The new Pyridazinone derivatives have been studied as vasorelaxant and antiplatelet agents. Analysis of biological data revealed the silyl ethers (4a-i) and N,O-dibenzyl derivatives (6g-i) as the most active compounds. © 2010 Elsevier Ltd. All rights reserved.
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pyridazines part 36 synthesis and antiplatelet activity of 5 substituted 6 phenyl 3 2h Pyridazinones
Bioorganic & Medicinal Chemistry Letters, 2004Co-Authors: Alberto Coelho, Eddy Sotelo, Nuria Fraiz, Matilde Yanez, Reyes Laguna, Ernesto Cano, Enrique RavinaAbstract:A convenient and efficient palladium-catalysed retro-ene-assisted method has been developed to prepare a series of 5-substituted-6-phenyl-3(2H)-Pyridazinones as potential antiplatelet drugs. The most active compounds were those that contain a 3-phenyl-3-oxo-propenyl fragment or a phenylthio group at position 5 of the heterocyclic ring.
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pyridazines part xxix synthesis and platelet aggregation inhibition activity of 5 substituted 6 phenyl 3 2h Pyridazinones novel aspects of their biological actions
Bioorganic & Medicinal Chemistry, 2002Co-Authors: Eddy Sotelo, Nuria Fraiz, Matilde Yanez, Reyes Laguna, Ernesto Cano, Vicente Terrades, Enrique RavinaAbstract:A series of 6-phenyl-3(2H)-Pyridazinones with a diverse range of substituents in the 5-position have been prepared and evaluated in the search for new antiplatelet agents. A significant dependence of the substituent on the inhibitory effect has been observed. The pharmacological study of these compounds confirms that modification of the chemical group at position 5 of the 6-phenyl-3(2H)-Pyridazinone system influences both variations in the antiplatelet activity and the mechanism of action.
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pyridazines part 28 5 alkylidene 6 phenyl 3 2h Pyridazinones a new family of platelet aggregation inhibitors
Bioorganic & Medicinal Chemistry Letters, 2002Co-Authors: Eddy Sotelo, Nuria Fraiz, Matilde Yanez, Reyes Laguna, Ernesto Cano, Jose Brea, Enrique RavinaAbstract:The synthesis and anti-platelet activity of several 5-alkylidene-6-phenyl-3(2H)-Pyridazinones are described. The most active compounds are those that contain oxygenated functions (COOR, COMe) on the alkylidene fragment (6a, 6b and 6c).
Zuxing Zhang - One of the best experts on this subject based on the ideXlab platform.
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synthesis fungicidal activity and 3d qsar of Pyridazinone substituted 1 3 4 oxadiazoles and 1 3 4 thiadiazoles
Journal of Agricultural and Food Chemistry, 2002Co-Authors: Zuxing ZhangAbstract:A series of novel 5-[1-aryl-1,4-dihydro-6-methylpyridazin-4-one-3-yl] -2-arylamino-1,3,4-oxadiazoles, fungicidally active, were synthesized based on bioisosterism and tested in vivo against wheat leaf rust, Puccinia recondita. These compounds were shown to be fungicidally active, and their activity was influenced by the nature of the substituents. By using the three-dimensional quantitative structure−activity relationships (3D-QSAR) method of comparative molecular field analysis (CoMFA), we have studied the structure and activity relationship of the compounds containing both Pyridazinone-substituted 1,3,4-thiadiazoles and Pyridazinone-substituted 1,3,4-oxadiazoles. The 3D-QSAR modes gave good correlation between the variations on percent inhibition and the steric-electrostatic properties. The results are consistent with a common mode of action for the Pyridazinone-substituted 1,3,4-thiadiazoles and the Pyridazinone-substituted 1,3,4-oxadiazoles, which further confirms that the 1,3,4-oxadiazole ring is a b...
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synthesis fungicidal activity and 3d qsar of Pyridazinone substituted 1 3 4 oxadiazoles and 1 3 4 thiadiazoles
Journal of Agricultural and Food Chemistry, 2002Co-Authors: Xiajuan Zou, Luhua Lai, Guiyu Jin, Zuxing ZhangAbstract:A series of novel 5-[1-aryl-1,4-dihydro-6-methylpyridazin-4-one-3-yl] -2-arylamino-1,3,4-oxadiazoles, fungicidally active, were synthesized based on bioisosterism and tested in vivo against wheat leaf rust, Puccinia recondita. These compounds were shown to be fungicidally active, and their activity was influenced by the nature of the substituents. By using the three-dimensional quantitative structure-activity relationships (3D-QSAR) method of comparative molecular field analysis (CoMFA), we have studied the structure and activity relationship of the compounds containing both Pyridazinone-substituted 1,3,4-thiadiazoles and Pyridazinone-substituted 1,3,4-oxadiazoles. The 3D-QSAR modes gave good correlation between the variations on percent inhibition and the steric-electrostatic properties. The results are consistent with a common mode of action for the Pyridazinone-substituted 1,3,4-thiadiazoles and the Pyridazinone-substituted 1,3,4-oxadiazoles, which further confirms that the 1,3,4-oxadiazole ring is a bioisosteric analogue of the 1,3,4-thiadiazole ring. These offer important structural insights into designing highly active compounds prior to their synthesis.
