The Experts below are selected from a list of 279 Experts worldwide ranked by ideXlab platform
Fan Wu - One of the best experts on this subject based on the ideXlab platform.
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a mild and efficient copper catalyzed coupling of aryl iodides and thiols using an Oxime phosphine oxide ligand
Tetrahedron Letters, 2006Co-Authors: Lei Xu, Fan WuAbstract:Abstract A mild and efficient copper-catalyzed system for the coupling of aryl iodides and thiols was developed using a readily prepared and highly stable Oxime–phosphine oxide ligand. Good to excellent yields were obtained.
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mild and efficient copper catalyzed n arylation of alkylamines and n h heterocycles using an Oxime phosphine oxide ligand
Tetrahedron, 2005Co-Authors: Lei Xu, Fan Wu, Rongliang WangAbstract:Abstract A mild and efficient copper-catalyzed system for N-arylation of alkylamines and N–H heterocycles with aryl iodides using a novel, readily prepared and highly stable Oxime-functionalized phosphine oxide ligand was developed. The coupling reactions could even be performed in solvent-free conditions with moderate to good yields.
Lei Xu - One of the best experts on this subject based on the ideXlab platform.
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a mild and efficient copper catalyzed coupling of aryl iodides and thiols using an Oxime phosphine oxide ligand
Tetrahedron Letters, 2006Co-Authors: Lei Xu, Fan WuAbstract:Abstract A mild and efficient copper-catalyzed system for the coupling of aryl iodides and thiols was developed using a readily prepared and highly stable Oxime–phosphine oxide ligand. Good to excellent yields were obtained.
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mild and efficient copper catalyzed n arylation of alkylamines and n h heterocycles using an Oxime phosphine oxide ligand
Tetrahedron, 2005Co-Authors: Lei Xu, Fan Wu, Rongliang WangAbstract:Abstract A mild and efficient copper-catalyzed system for N-arylation of alkylamines and N–H heterocycles with aryl iodides using a novel, readily prepared and highly stable Oxime-functionalized phosphine oxide ligand was developed. The coupling reactions could even be performed in solvent-free conditions with moderate to good yields.
Rongliang Wang - One of the best experts on this subject based on the ideXlab platform.
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mild and efficient copper catalyzed n arylation of alkylamines and n h heterocycles using an Oxime phosphine oxide ligand
Tetrahedron, 2005Co-Authors: Lei Xu, Fan Wu, Rongliang WangAbstract:Abstract A mild and efficient copper-catalyzed system for N-arylation of alkylamines and N–H heterocycles with aryl iodides using a novel, readily prepared and highly stable Oxime-functionalized phosphine oxide ligand was developed. The coupling reactions could even be performed in solvent-free conditions with moderate to good yields.
John R Cashman - One of the best experts on this subject based on the ideXlab platform.
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Nonquaternary reactivators for organophosphate-inhibited cholinesterases
Journal of Medicinal Chemistry, 2012Co-Authors: Jarosław Kalisiak, Erik C. Ralph, John R CashmanAbstract:A new class of amidine-Oxime reactivators of organophosphate (OP)-inhibited cholinesterases (ChE) was synthesized and tested in vitro and in vivo. Compared with 2-PAM, the most promising cyclic amidine-Oxime (i.e., 12e) showed comparable or greater reactivation of OP-inactivated AChE and OP-inactivated BChE. To the best of our knowledge, this is the first report of a nonquaternary Oxime that has, comparable to 2-PAM, in vitro potency for reactivation of Sarin (GB)-inhibited AChE and BChE. Amidine-Oximes were tested in vitro, and reactivation rates for OP-inactivated butyrylcholinesterase (BChE) were greater than those for 2-PAM or MINA. Amidine-Oxime reactivation rates for OP-inactivated acetylcholinesterase (AChE) were lower compared to 2-PAM but greater compared with MINA. Amidine-Oximes were tested in vivo for protection against the toxicity of nerve agent model compounds. (i.e., a model of Sarin). Post-treatment (i.e., 5 min after OP exposure, i.p,) with amidine Oximes 7a-c and 12a, 12c, 12e, 12f, and 15b (145 μmol/kg, i.p.) protected 100% of the mice challenged with the sarin model compound. Even at 25% of the initial dose of amidine-Oxime (i.e., a dose of 36 μmol/kg, i.p.), 7b and 12e protected 100% of the animals challenged with the sarin nerve agent model compound that caused lethality in 6/11 animals without amidine-Oxime.
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Amidine-Oximes: reactivators for organophosphate exposure.
Journal of Medicinal Chemistry, 2011Co-Authors: Jarosław Kalisiak, Erik C. Ralph, Jun Zhang, John R CashmanAbstract:A new class of amidine−Oxime reactivators of organophosphate (OP)-inhibited cholinesterases (ChE) were designed, synthesized, and tested. These compounds represent a novel group of Oximes with enhanced capabilities of crossing the blood−brain barrier. Lack of brain penetration is a major limitation for currently used Oximes as antidotes of OP poisoning. The concept described herein relies on a combination of an amidine residue and Oxime functionality whereby the amidine increases the binding affinity to the ChE and the Oxime is responsible for reactivation. Amidine−Oximes were tested in vitro and reactivation rates for OP-BuChE were greater than pralidOxime (2-PAM) or monoisonitrosoacetone (MINA). Amidine−Oxime reactivation rates for OP-AChE were lower compared to 2-PAM but greater compared with MINA. After pretreatment for 30 min with Oximes 15c and 15d (145 μmol/kg, ip) mice were challenged with a soman model compound. In addition, 15d was tested in a post-treatment experiment (145 μmol/kg, ip, administ...
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Amidine-Oximes: Reactivators for organophosphate exposure
Journal of Medicinal Chemistry, 2011Co-Authors: Jarosław Kalisiak, Erik C. Ralph, Jun Zhang, John R CashmanAbstract:A new class of amidine-Oxime reactivators of organophosphate (OP)-inhibited cholinesterases (ChE) were designed, synthesized, and tested. These compounds represent a novel group of Oximes with enhanced capabilities of crossing the blood-brain barrier. Lack of brain penetration is a major limitation for currently used Oximes as antidotes of OP poisoning. The concept described herein relies on a combination of an amidine residue and Oxime functionality whereby the amidine increases the binding affinity to the ChE and the Oxime is responsible for reactivation. Amidine-Oximes were tested in vitro and reactivation rates for OP-BuChE were greater than pralidOxime (2-PAM) or monoisonitrosoacetone (MINA). Amidine-Oxime reactivation rates for OP-AChE were lower compared to 2-PAM but greater compared with MINA. After pretreatment for 30 min with Oximes 15c and 15d (145 μmol/kg, ip) mice were challenged with a soman model compound. In addition, 15d was tested in a post-treatment experiment (145 μmol/kg, ip, administration 5 min after sarin model compound exposure). In both cases, amidine-Oximes afforded 100% 24 h survival in an animal model of OP exposure.
Jane Robertson - One of the best experts on this subject based on the ideXlab platform.
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Oximes for acute organophosphate pesticide poisoning
Cochrane Database of Systematic Reviews, 2011Co-Authors: N A Buckley, Marc Bevan, Michael Eddleston, Yi Li, Jane RobertsonAbstract:Acute organophosphorus pesticide poisoning causes tens of thousands of deaths each year across the developing world. Standard treatment involves administration of intravenous atropine and Oxime to reactivate inhibited acetylcholinesterase. The clinical usefulness of Oximes, such as pralidOxime and obidOxime, has been challenged over the past 20 years by physicians in many parts of the world.