Publications by authors named "Pascal George"

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Chemical, Biochemical, Cellular, and Physiological Characterization of Leucettinib-21, a Down Syndrome and Alzheimer's Disease Drug Candidate.
Mattias F Lindberg, Emmanuel Deau, Frédéric Miege, Marie Greverie, Didier Roche, Nicolas George, Pascal George

J Med Chem· December 2023

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Leucettinibs, a Class of DYRK/CLK Kinase Inhibitors Inspired by the Marine Sponge Natural Product Leucettamine B.
Emmanuel Deau, Mattias F Lindberg, Frédéric Miege, Didier Roche, Nicolas George, Pascal George

J Med Chem· August 2023

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Comparative Efficacy and Selectivity of Pharmacological Inhibitors of DYRK and CLK Protein Kinases.
Mattias F Lindberg, Emmanuel Deau, Jonas Arfwedson, Nicolas George, Pascal George

J Med Chem· March 2023

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Discovery and Optimization of Potent and Orally Available CTP Synthetase Inhibitors for Use in Treatment of Diseases Driven by Aberrant Immune Cell Proliferation.
Andrew Novak, David Laughton, Rebecca Lane, Emma Blackham, Jennifer Thomas, Pascal George

J Med Chem· December 2022

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Design and synthesis of a novel series of histamine H3 receptor antagonists through a scaffold hopping strategy.
Zhongli Gao, William J Hurst, Daniel Hall, Ryan Hartung, William Reynolds, Pascal G George

Bioorg Med Chem· February 2015

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Selective blockade of the hydrolysis of the endocannabinoid 2-arachidonoylglycerol impairs learning and memory performance while producing antinociceptive activity in rodents.
Guy Griebel, Philippe Pichat, Sandra Beeské, Thibaud Leroy, Nicolas Redon, Pascal George

Sci Rep· January 2015

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Interfacing chemical biology and drug discovery: report from the 50th International Conference on Medicinal Chemistry of the SCT (French Medicinal Chemistry Society), July 2-4, 2014, Rouen, France.
Janos Sapi, Frédéric Schmidt, Luc Van Hijfte, Pascal George

ACS Chem Biol· December 2014

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Chemical biology: contribution to molecular therapeutic innovation--a new role for chemistry? Report from the thematic symposium organized by the SCT (French Medicinal Chemistry Society), November 26th, 2013.
Frédéric Schmidt, Pascal George, Janos Sapi

ACS Chem Biol· April 2014

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Identification and profiling of 3,5-dimethyl-isoxazole-4-carboxylic acid [2-methyl-4-((2S,3'S)-2-methyl-[1,3']bipyrrolidinyl-1'-yl)phenyl] amide as histamine H(3) receptor antagonist for the treatment of depression.
Zhongli Gao, William J Hurst, Werngard Czechtizky, Daniel Hall, Nicolas Moindrot, Pascal G George

Bioorg Med Chem Lett· December 2013

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Discovery of a potent, selective, and orally bioavailable histamine H3 receptor antagonist SAR110068 for the treatment of sleep-wake disorders.
Zhongli Gao, William J Hurst, Werngard Czechtizky, Dominique Francon, Guy Griebel, Pascal G George

Bioorg Med Chem Lett· November 2013

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Synthesis, characterization, and biological assessment of the four stereoisomers of the H(3) receptor antagonist 5-fluoro-2-methyl-N-[2-methyl-4-(2-methyl[1,3']bipyrrolidinyl-1'-yl)phenyl]benzamide.
Zhongli Gao, William J Hurst, Etienne Guillot, Raisa Nagorny, Marie-Pierre Pruniaux, Pascal G George

Bioorg Med Chem Lett· July 2013

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Discovery of aryl ureas and aryl amides as potent and selective histamine H3 receptor antagonists for the treatment of obesity (part I).
Zhongli Gao, William J Hurst, Etienne Guillot, Werngard Czechtizky, Ulrike Lukasczyk, Pascal G George

Bioorg Med Chem Lett· June 2013

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Discovery of aryl ureas and aryl amides as potent and selective histamine H3 receptor antagonists for the treatment of obesity (part II).
Zhongli Gao, William J Hurst, Etienne Guillot, Werngard Czechtizky, Ulrike Lukasczyk, Pascal G George

Bioorg Med Chem Lett· June 2013

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Ring expansion of cyclic β-amino alcohols induced by diethylaminosulfur trifluoride: synthesis of cyclic amines with a tertiary fluorine at C3.
Bruno Anxionnat, Benoit Robert, Pascal George, Gino Ricci, Marc-Antoine Perrin

J Org Chem· July 2012

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Synthesis of aminopyridines and aminopyridones by cobalt-catalyzed [2+2+2] cycloadditions involving yne-ynamides: scope, limitations, and mechanistic insights.
Pierre Garcia, Yannick Evanno, Pascal George, Mireille Sevrin, Gino Ricci

Chemistry· April 2012

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Synthesis and biological evaluation of analogues of M6G.
Claire Trécant, Alain Dlubala, Pascal George, Philippe Pichat, Isabelle Ripoche

Eur J Med Chem· September 2011

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Regioselective cobalt-catalyzed formation of bicyclic 3- and 4-aminopyridines.
Pierre Garcia, Yannick Evanno, Pascal George, Mireille Sevrin, Gino Ricci

Org Lett· April 2011

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In vivo quantification of monoamine oxidase A in baboon brain: a PET study using [(11)C]befloxatone and the multi-injection approach.
Michel Bottlaender, Héric Valette, Jacques Delforge, Wadad Saba, Ilonka Guenther, Pascal George

J Cereb Blood Flow Metab· April 2010

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[(11)C]SL25.1188, a new reversible radioligand to study the monoamine oxidase type B with PET: preclinical characterisation in nonhuman primate.
Wadad Saba, Héric Valette, Marie-Anne Peyronneau, Yann Bramoullé, Christine Coulon, Pascal George

Synapse· January 2010

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Characterization of SSR103800, a selective inhibitor of the glycine transporter-1 in models predictive of therapeutic activity in schizophrenia.
Denis Boulay, Philippe Pichat, Gihad Dargazanli, Genevieve Estenne-Bouhtou, Jean Paul Terranova, Pascal George

Pharmacol Biochem Behav· November 2008

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SSR180711, a novel selective alpha7 nicotinic receptor partial agonist: (1) binding and functional profile.
Bruno Biton, Olivier E Bergis, Frédéric Galli, Alain Nedelec, Alistair W Lochead, Pascal George

Neuropsychopharmacology· January 2007

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Neurochemical, electrophysiological and pharmacological profiles of the selective inhibitor of the glycine transporter-1 SSR504734, a potential new type of antipsychotic.
Ronan Depoortère, Gihad Dargazanli, Genevieve Estenne-Bouhtou, Annick Coste, Christophe Lanneau, Pascal George

Neuropsychopharmacology· November 2005

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Synthesis of new potentially bioactive bicyclic 2-pyridones.
Maxime D Crozet, Pascal George, Michel P Crozet, Patrice Vanelle

Molecules· October 2005

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Solid-phase syntheses of 6-arylpyridazin-3(2H)-ones.
Richard Salives, Georges Dupas, Nelly Plé, Guy Quéguiner, Alain Turck, Pascal George

J Comb Chem· July 2005

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Design and synthesis of novel imidazo[1,2-a]quinoxalines as PDE4 inhibitors.
Carine Deleuze-Masquéfa, Grégori Gerebtzoff, Guy Subra, Jean-Roch Fabreguettes, Annabel Ovens, Pascal George

Bioorg Med Chem· March 2004

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