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Fabien Gosselet - One of the best experts on this subject based on the ideXlab platform.
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chemoselective hydrogenation of 6 alkynyl 3 fluoro 2 pyridinaldoximes access to first in class 6 alkyl 3 fluoro 2 pyridinaldoxime scaffolds as new reactivators of sarin inhibited human acetylcholinesterase with increased blood brain barrier permeability
Chemistry: A European Journal, 2020Co-Authors: Jagadeesh Yerri, Jose A Dias, Mallikajurna Reddy Nimmakayala, Franck Razafindrainibe, Charlotte Courageux, Annejulie Gastellier, Johanne Jegoux, Caroline Coisne, Christophe Landry, Fabien GosseletAbstract:Novel 6-alkyl- and 6-alkenyl-3-fluoro-2-pyridinaldoximes have been synthesised by using a mild and efficient chemoselective hydrogenation of 6-alkynyl-3-fluoro-2-pyridinaldoxime scaffolds, without altering the reducible, unprotected, sensitive oxime functionality and the C-F bond. These novel 6-alkyl-3-fluoro-2-pyridinaldoximes may find medicinal application as antidotes to organophosphate poisoning. Indeed, one Low-Molecular-Weight Compound exhibited increased affinity for sarin-inhibited acetylcholinesterase (hAChE) and greater reactivation efficiency or resurrection for sarin-inhibited hAChE, compared with those of 2-pyridinaldoxime (2-PAM) and 1-({[4-(aminocarbonyl)pyridinio]methoxy}methyl)-2-[(hydroxyimino)methyl]pyridinium chloride (HI-6), two pyridinium salts currently used as antidote by several countries. In addition, the uncharged 3-fluorinated bifunctional hybrid showed increased in vitro blood-brain barrier permeability compared with those of 2-PAM, HI-6 and obidoxime. These promising features of novel Low-Molecular-Weight alkylfluoropyridinaldoxime open up a new era for the design, synthesis and discovery of central non-quaternary broad spectrum reactivators for organophosphate-inhibited cholinesterases.
Jagadeesh Yerri - One of the best experts on this subject based on the ideXlab platform.
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chemoselective hydrogenation of 6 alkynyl 3 fluoro 2 pyridinaldoximes access to first in class 6 alkyl 3 fluoro 2 pyridinaldoxime scaffolds as new reactivators of sarin inhibited human acetylcholinesterase with increased blood brain barrier permeability
Chemistry: A European Journal, 2020Co-Authors: Jagadeesh Yerri, Jose A Dias, Mallikajurna Reddy Nimmakayala, Franck Razafindrainibe, Charlotte Courageux, Annejulie Gastellier, Johanne Jegoux, Caroline Coisne, Christophe Landry, Fabien GosseletAbstract:Novel 6-alkyl- and 6-alkenyl-3-fluoro-2-pyridinaldoximes have been synthesised by using a mild and efficient chemoselective hydrogenation of 6-alkynyl-3-fluoro-2-pyridinaldoxime scaffolds, without altering the reducible, unprotected, sensitive oxime functionality and the C-F bond. These novel 6-alkyl-3-fluoro-2-pyridinaldoximes may find medicinal application as antidotes to organophosphate poisoning. Indeed, one Low-Molecular-Weight Compound exhibited increased affinity for sarin-inhibited acetylcholinesterase (hAChE) and greater reactivation efficiency or resurrection for sarin-inhibited hAChE, compared with those of 2-pyridinaldoxime (2-PAM) and 1-({[4-(aminocarbonyl)pyridinio]methoxy}methyl)-2-[(hydroxyimino)methyl]pyridinium chloride (HI-6), two pyridinium salts currently used as antidote by several countries. In addition, the uncharged 3-fluorinated bifunctional hybrid showed increased in vitro blood-brain barrier permeability compared with those of 2-PAM, HI-6 and obidoxime. These promising features of novel Low-Molecular-Weight alkylfluoropyridinaldoxime open up a new era for the design, synthesis and discovery of central non-quaternary broad spectrum reactivators for organophosphate-inhibited cholinesterases.
Charlotte Courageux - One of the best experts on this subject based on the ideXlab platform.
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chemoselective hydrogenation of 6 alkynyl 3 fluoro 2 pyridinaldoximes access to first in class 6 alkyl 3 fluoro 2 pyridinaldoxime scaffolds as new reactivators of sarin inhibited human acetylcholinesterase with increased blood brain barrier permeability
Chemistry: A European Journal, 2020Co-Authors: Jagadeesh Yerri, Jose A Dias, Mallikajurna Reddy Nimmakayala, Franck Razafindrainibe, Charlotte Courageux, Annejulie Gastellier, Johanne Jegoux, Caroline Coisne, Christophe Landry, Fabien GosseletAbstract:Novel 6-alkyl- and 6-alkenyl-3-fluoro-2-pyridinaldoximes have been synthesised by using a mild and efficient chemoselective hydrogenation of 6-alkynyl-3-fluoro-2-pyridinaldoxime scaffolds, without altering the reducible, unprotected, sensitive oxime functionality and the C-F bond. These novel 6-alkyl-3-fluoro-2-pyridinaldoximes may find medicinal application as antidotes to organophosphate poisoning. Indeed, one Low-Molecular-Weight Compound exhibited increased affinity for sarin-inhibited acetylcholinesterase (hAChE) and greater reactivation efficiency or resurrection for sarin-inhibited hAChE, compared with those of 2-pyridinaldoxime (2-PAM) and 1-({[4-(aminocarbonyl)pyridinio]methoxy}methyl)-2-[(hydroxyimino)methyl]pyridinium chloride (HI-6), two pyridinium salts currently used as antidote by several countries. In addition, the uncharged 3-fluorinated bifunctional hybrid showed increased in vitro blood-brain barrier permeability compared with those of 2-PAM, HI-6 and obidoxime. These promising features of novel Low-Molecular-Weight alkylfluoropyridinaldoxime open up a new era for the design, synthesis and discovery of central non-quaternary broad spectrum reactivators for organophosphate-inhibited cholinesterases.
Franck Razafindrainibe - One of the best experts on this subject based on the ideXlab platform.
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chemoselective hydrogenation of 6 alkynyl 3 fluoro 2 pyridinaldoximes access to first in class 6 alkyl 3 fluoro 2 pyridinaldoxime scaffolds as new reactivators of sarin inhibited human acetylcholinesterase with increased blood brain barrier permeability
Chemistry: A European Journal, 2020Co-Authors: Jagadeesh Yerri, Jose A Dias, Mallikajurna Reddy Nimmakayala, Franck Razafindrainibe, Charlotte Courageux, Annejulie Gastellier, Johanne Jegoux, Caroline Coisne, Christophe Landry, Fabien GosseletAbstract:Novel 6-alkyl- and 6-alkenyl-3-fluoro-2-pyridinaldoximes have been synthesised by using a mild and efficient chemoselective hydrogenation of 6-alkynyl-3-fluoro-2-pyridinaldoxime scaffolds, without altering the reducible, unprotected, sensitive oxime functionality and the C-F bond. These novel 6-alkyl-3-fluoro-2-pyridinaldoximes may find medicinal application as antidotes to organophosphate poisoning. Indeed, one Low-Molecular-Weight Compound exhibited increased affinity for sarin-inhibited acetylcholinesterase (hAChE) and greater reactivation efficiency or resurrection for sarin-inhibited hAChE, compared with those of 2-pyridinaldoxime (2-PAM) and 1-({[4-(aminocarbonyl)pyridinio]methoxy}methyl)-2-[(hydroxyimino)methyl]pyridinium chloride (HI-6), two pyridinium salts currently used as antidote by several countries. In addition, the uncharged 3-fluorinated bifunctional hybrid showed increased in vitro blood-brain barrier permeability compared with those of 2-PAM, HI-6 and obidoxime. These promising features of novel Low-Molecular-Weight alkylfluoropyridinaldoxime open up a new era for the design, synthesis and discovery of central non-quaternary broad spectrum reactivators for organophosphate-inhibited cholinesterases.
Mallikajurna Reddy Nimmakayala - One of the best experts on this subject based on the ideXlab platform.
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chemoselective hydrogenation of 6 alkynyl 3 fluoro 2 pyridinaldoximes access to first in class 6 alkyl 3 fluoro 2 pyridinaldoxime scaffolds as new reactivators of sarin inhibited human acetylcholinesterase with increased blood brain barrier permeability
Chemistry: A European Journal, 2020Co-Authors: Jagadeesh Yerri, Jose A Dias, Mallikajurna Reddy Nimmakayala, Franck Razafindrainibe, Charlotte Courageux, Annejulie Gastellier, Johanne Jegoux, Caroline Coisne, Christophe Landry, Fabien GosseletAbstract:Novel 6-alkyl- and 6-alkenyl-3-fluoro-2-pyridinaldoximes have been synthesised by using a mild and efficient chemoselective hydrogenation of 6-alkynyl-3-fluoro-2-pyridinaldoxime scaffolds, without altering the reducible, unprotected, sensitive oxime functionality and the C-F bond. These novel 6-alkyl-3-fluoro-2-pyridinaldoximes may find medicinal application as antidotes to organophosphate poisoning. Indeed, one Low-Molecular-Weight Compound exhibited increased affinity for sarin-inhibited acetylcholinesterase (hAChE) and greater reactivation efficiency or resurrection for sarin-inhibited hAChE, compared with those of 2-pyridinaldoxime (2-PAM) and 1-({[4-(aminocarbonyl)pyridinio]methoxy}methyl)-2-[(hydroxyimino)methyl]pyridinium chloride (HI-6), two pyridinium salts currently used as antidote by several countries. In addition, the uncharged 3-fluorinated bifunctional hybrid showed increased in vitro blood-brain barrier permeability compared with those of 2-PAM, HI-6 and obidoxime. These promising features of novel Low-Molecular-Weight alkylfluoropyridinaldoxime open up a new era for the design, synthesis and discovery of central non-quaternary broad spectrum reactivators for organophosphate-inhibited cholinesterases.
