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authFullName_s : Florian Nachon

Multi-target-directed ligands for treating Alzheimer's disease: Butyrylcholinesterase inhibitors displaying antioxidant and neuroprotective activities

Damijan Knez , Nicolas Coquelle , Anja Pišlar , Simon Žakelj , Marko Jukič et al.
European Journal of Medicinal Chemistry, 2018, 156, pp.598 - 617. ⟨10.1016/j.ejmech.2018.07.033⟩
Journal articles hal-01924686v1

Relation between dynamics, activity and thermal stability within the cholinesterase family

Marie Trovaslet , Marcus Trapp , Martin Weik , Florian Nachon , Patrick Masson et al.
Chemico-Biological Interactions, 2013, 203 (1), pp.14 - 18. ⟨10.1016/j.cbi.2012.08.004⟩
Journal articles hal-01664592v1

First efficient uncharged reactivators for the dephosphylation of poisoned human acetylcholinesterase.

Guillaume Mercey , Tristan Verdelet , Géraldine Saint-André , Emilie Gillon , Alain Wagner et al.
Chemical Communications, 2011, 47 (18), pp.5295-5297. ⟨10.1039/c1cc10787a⟩
Journal articles hal-00991912v1

Syntheses and in vitro evaluations of uncharged reactivators for human acetylcholinesterase inhibited by organophosphorus nerve agents.

Julien Renou , Guillaume Mercey , Tristan Verdelet , Emilia Păunescu , Emilie Gillon et al.
Chemico-Biological Interactions, 2013, 203 (1), pp.81-84. ⟨10.1016/j.cbi.2012.09.023⟩
Journal articles hal-00996535v1

The Magic of Crystal Structure-Based Inhibitor Optimization: Development of a Butyrylcholinesterase Inhibitor with Picomolar Affinity and in Vivo Activity

Urban Košak , Boris Brus , Damijan Knez , Simon Žakelj , Jurij Trontelj et al.
Journal of Medicinal Chemistry, 2018, 61 (1), pp.119-139. ⟨10.1021/acs.jmedchem.7b01086⟩
Journal articles hal-01991973v1

N-Propargylpiperidines with naphthalene-2-carboxamide or naphthalene-2-sulfonamide moieties: Potential multifunctional anti-Alzheimer's agents.

Urban Košak , Damijan Knez , Nicolas Coquelle , Boris Brus , Anja Pišlar et al.
Bioorganic and Medicinal Chemistry, 2017, 25 (2), pp.633-645. ⟨10.1016/j.bmc.2016.11.032⟩
Journal articles hal-01465675v1

Huprine derivatives as sub-nanomolar human acetylcholinesterase inhibitors: from rational design to validation by X-ray crystallography.

Cyril Ronco , Eugénie Carletti , Jacques-Philippe Colletier , Martin Weik , Florian Nachon et al.
ChemMedChem, 2012, 7 (3), pp.400-405. ⟨10.1002/cmdc.201100438⟩
Journal articles istex hal-00996475v1

Design, synthesis and biological evaluation of novel tetrahydroacridine pyridine- aldoxime and -amidoxime hybrids as efficient uncharged reactivators of nerve agent-inhibited human acetylcholinesterase

Maria Kliachyna , Gianluca Santoni , Valentin Nussbaum , Julien Renou , Benoît Sanson et al.
European Journal of Medicinal Chemistry, 2014, 78, pp.455-467. ⟨10.1016/j.ejmech.2014.03.044⟩
Journal articles hal-01131268v1

Discovery of a Potent Dual Inhibitor of Acetylcholinesterase and Butyrylcholinesterase with Antioxidant Activity that Alleviates Alzheimer-like Pathology in Old APP/PS1 Mice

Elisabet Viayna , Nicolas Coquelle , Monika Cieslikiewicz-Bouet , Pedro Cisternas , Carolina Oliva et al.
Journal of Medicinal Chemistry, 2020, ⟨10.1021/acs.jmedchem.0c01775⟩
Journal articles hal-03094189v1
Image document

Respiratory failure triggered by cholinesterase inhibitors may involve activation of a reflex sensory pathway by acetylcholine spillover

Aurélie Nervo , André-Guilhem Calas , Florian Nachon , Eric Krejci
Toxicology, 2019, 424, pp.152232. ⟨10.1016/j.tox.2019.06.003⟩
Journal articles hal-02323726v1

Reactivators of acetylcholinesterase inhibited by organophosphorus nerve agents

Guillaume Mercey , Tristan Verdelet , Julien Renou , Maria Kliachyna , Rachid Baati et al.
Accounts of Chemical Research, 2012, 45 (5), pp.756-766. ⟨10.1021/ar2002864⟩
Journal articles hal-01015972v1
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Apport des structures cristallographiques à la compréhension du mécanisme d'inhibition des cholinestérases par les neurotoxiques organophosphorés

Florian Nachon
Biologie structurale [q-bio.BM]. Université Joseph Fourier, 2014
Habilitation à diriger des recherches tel-01287758v1

Potent 3‐Hydroxy‐2‐Pyridine Aldoxime Reactivators of Organophosphate‐Inhibited Cholinesterases with Predicted Blood–Brain Barrier Penetration

Tamara Zorbaz , Anissa Braïki , Nikola Marakovic , Julien Renou , Eugenio de La Mora et al.
Chemistry - A European Journal, 2018, 24 (38), pp.9675-9691. ⟨10.1002/chem.201801394⟩
Journal articles hal-02024542v1

Dynamics of human acetylcholinesterase bound to non-covalent and covalent inhibitors shedding light on changes to the water network structure

Judith Peters , Nicolas Martinez , Marie Trovaslet , Kévin Scannapieco , Michael Marek Koza et al.
Physical Chemistry Chemical Physics, 2016, 18 (18), pp.12992-13001
Journal articles hal-02002944v1

Synthesis and structure–activity relationship of Huprine derivatives as human acetylcholinesterase inhibitors

Cyril Ronco , Geoffroy Sorin , Florian Nachon , Richard Foucault , Ludovic Jean et al.
Bioorganic & Medicinal Chemistry Letters, 2009, 17 (13), pp.4523-4536. ⟨10.1016/j.bmc.2009.05.005⟩
Journal articles hal-03808202v1

Development of an in-vivo active reversible butyrylcholinesterase inhibitor.

Urban Košak , Boris Brus , Damijan Knez , Roman Šink , Simon Žakelj et al.
Scientific Reports, 2016, 6, pp.39495. ⟨10.1038/srep39495⟩
Journal articles hal-01465678v1

Crystal structures of human cholinesterases in complex with huprine W and tacrine: elements of specificity for anti-Alzheimer's drugs targeting acetyl- and butyryl-cholinesterase.

Florian Nachon , Eugénie Carletti , Cyril Ronco , Marie Trovaslet , Yvain Nicolet et al.
Biochemical Journal, 2013, 453 (3), pp.393-399. ⟨10.1042/BJ20130013⟩
Journal articles hal-00996550v1

Synthesis and in vitro and in vivo evaluations of New Uncharged reactivators for cholinesterases inhibited by organophosphorus nerve agents

Anissa Braïki , Julien Renou , Romain Mougeot , Florian Nachon , José Dias et al.
Medical Chemical Defense Conference (MCDC, 17, 2019), Mar 2019, Munich, Germany
Conference poster hal-02543452v1

Correlation of the dynamics of native human acetylcholinesterase and its inhibited huperzine A counterpart from sub-picoseconds to nanoseconds.

M Trapp , M Tehei , Marie Trovaslet , Florian Nachon , Nicolas Martinez et al.
Journal of the Royal Society Interface, 2014, 11 (97), pp.20140372
Journal articles hal-01131840v1

Composition and methods for the purification and production of butyrylcholinesterase.

O. Lockridge, , M.A. Larson, , S.H. Schopfer, , S.H. Hinrichs, , Florian Nachon et al.
France, Patent n° : PCT/US14/66373. 2014
Patents hal-01150306v1

Tryptoline-​3-​hydroxypyridinaldoxime conjugates as efficient reactivators of phosphylated human acetyl and butyrylcholinesterase

Julien Renou , Melanie Loiodice , Melanie Arboleas , Rachid Baati , Ludovic Jean et al.
Chemical Communications, 2014, 50 (30), pp.3947-3950. ⟨10.1039/C4CC00561A⟩
Journal articles hal-01150284v1
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A New Class of Bi- and Trifunctional Sugar Oximes as Antidotes against Organophosphorus Poisoning

Ophélie da Silva , Nicolas Probst , Christophe Landry , Anne-Sophie Hanak , Pierre Warnault et al.
Journal of Medicinal Chemistry, 2022, 65 (6), pp.4649-4666. ⟨10.1021/acs.jmedchem.1c01748⟩
Journal articles hal-03706969v1

Preparation of 7,​11-​Methanocycloocta[b]​quinoline derivative as highly functionalizable acetylcholinesterase inhibitors for treating neurological diseases

Cyril Ronco , Pierre-Yves Renard , Ludovic Jean , Florian Nachon , Anthony Romieu et al.
France, Patent n° : WO 2011124712 A1. 2011
Patents hal-01150301v1

An easy method for the determination of active concentrations of cholinesterase reactivators in blood samples: Application to the efficacy assessment of non quaternary reactivators compared to HI-6 and pralidoxime in VX-poisoned mice

André-Guilhem Calas , José Dias , Catherine Rousseau , Mélanie Arboléas , Mélanie Touvrey-Loiodice et al.
Chemico-Biological Interactions, 2017, 267 (1), pp.11-16. ⟨10.1016/j.cbi.2016.03.009⟩
Journal articles hal-02046266v1

New huprine derivatives functionalized at position 9 as highly potent acetylcholinesterase inhibitors.

Cyril Ronco , Richard Foucault , Emilie Gillon , Pierre Bohn , Florian Nachon et al.
ChemMedChem, 2011, 6 (5), pp.876-888. ⟨10.1002/cmdc.201000523⟩
Journal articles istex hal-00991920v1
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Efficacy Assessment of an Uncharged Reactivator of NOP-Inhibited Acetylcholinesterase Based on Tetrahydroacridine Pyridine-Aldoxime Hybrid in Mouse Compared to Pralidoxime

André-Guilhem Calas , Anne-Sophie Hanak , Nina Jaffré , Aurélie Nervo , José Dias et al.
Biomolecules, 2020, 10 (6), pp.858. ⟨10.3390/biom10060858⟩
Journal articles hal-03127255v1
Image document

On the Influence of the Protonation States of Active Site Residues on AChE Reactivation: A QM/MM Approach

Thomas Driant , Florian Nachon , Cyril Ollivier , Pierre-Yves Renard , Etienne Derat et al.
ChemBioChem, 2017, 18 (7), pp.666-675. ⟨10.1002/cbic.201600646⟩
Journal articles hal-01644385v1

Reaction site-driven regioselective synthesis of AChE inhibitors

Emilia Oueis , Gianluca Santoni , Cyril Ronco , Olga A. Syzgantseva , Vincent Tognetti et al.
Organic & Biomolecular Chemistry, 2014, 12 (1), pp.156-161. ⟨10.1039/C3OB42109K⟩
Journal articles hal-02335933v1

Synthesis and in vitro evaluation of donepezil-based reactivators and analogues for nerve agent-inhibited human acetylcholinesterase

Julien Renou , José Dias , Guillaume Mercey , Tristan Verdelet , Catherine Rousseau et al.
RSC Advances, 2016, 6 (22), pp.17929-17940. ⟨10.1039/c5ra25477a⟩
Journal articles hal-02046237v1

Uncharged reactivators of cholinesterases inhibited by organophosphorus nerve agents.

Nicolas Probst , Anissa Braïki , Pierre Warnault , Julien Renou , Catherine Gomez et al.
International Meeting on Cholinesterases (13, 2018) and International Conference on Paraoxonases (7, 2018)), Sep 2018, Hradec Králové, Czech Republic
Conference poster hal-02543467v1