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nicolas Willand

Professeur des universités CNU : SECTION 86 - SCIENCES DU MÉDICAMENT ET DES AUTRES PRODUITS DE SANTÉ Laboratoire / équipe

Publications

hal-04625214

Thibault Caradec, Coline Ple, Giuseppe Sicoli, Ravil Petrov, Elizabeth Pradel, Cécilia Sobieski, Rudy Antoine, Maylis Orio, Adrien Herledan, Nicolas Willand, Ruben Hartkoorn

Small molecule MarR modulators potentiate metronidazole antibiotic activity in aerobic E. coli by inducing activation by the nitroreductase NfsA.

Journal of Biological Chemistry, 2024, J Biol Chem, pp.107431. ⟨10.1016/j.jbc.2024.107431⟩

hal-04093378

Francesca Ruggieri, Nina Compagne, Kevin Antraygues, Maxime Eveque, Marion Flipo, Nicolas Willand

Antibiotics with novel mode of action as new weapons to fight antimicrobial resistance

European Journal of Medicinal Chemistry, 2023, 256, pp.115413. ⟨10.1016/j.ejmech.2023.115413⟩

hal-04562021

Juan Rodriguez Mosheim, Francesca Ruggieri, Catherine Humeau, Philippe Hance, Nicolas Willand, Jean-Louis Hilbert, Egon Heuson, Renato Froidevaux

BIOCATALYTIC APPROACH TO CHEMOSELECTIVE ACYLATION OF SESQUITERPENE LACTONES FROM CHICORY: TOWARDS NEW ESTERS

BIOTRANS, Jun 2023, La Rochelle, France

hal-04007450

Léo Faïon, Kamel Djaout, Catalin Pintiala, Catherine Piveteau, Florence Leroux, Alexandre Biela, Stéphanie Slupek, Rudy Antoine, Monika Záhorszká, Francois-Xavier Cantrelle, Xavier Hanoulle, Jana Korduláková, Benoit Deprez, Nicolas Willand, Alain Baulard, Marion Flipo

Exploring the Antitubercular Activity of Anthranilic Acid Derivatives: From MabA (FabG1) Inhibition to Intrabacterial Acidification

Pharmaceuticals, 2023, 16 (3), pp.335. ⟨10.3390/ph16030335⟩

hal-04017312

Kevin Antraygues, Mathieu Maingot, Birgit Schellhorn, Vincent Trebosc, Marc Gitzinger, Benoit Déprez, Olivier Defert, Glenn E Dale, Marilyne Bourotte, Sergio Lociuro, Nicolas Willand

Design and synthesis of water-soluble prodrugs of rifabutin for intraveneous administration

European Journal of Medicinal Chemistry, 2022, 238, pp.114515. ⟨10.1016/j.ejmech.2022.114515⟩

hal-03969988

Benjamin Guieu, Jean-Pierre Jourdan, Aurore Dreneau, Nicolas Willand, Christophe Rochais, Patrick Dallemagne

Desirable drug–drug interactions or when a matter of concern becomes a renewed therapeutic strategy

Drug Discovery Today, 2021, 26 (2), pp.315-328. ⟨10.1016/j.drudis.2020.11.026⟩

hal-04465890

Benoit Deprez, Damien Bosc, Julie Charton, Cyril Couturier, Rebecca Deprez-Poulain, Marion Flipo, Florence Leroux, Baptiste Villemagne, Nicolas Willand

Molecular Design in Practice: A Review of Selected Projects in a French Research Institute That Illustrates the Link between Chemical Biology and Medicinal Chemistry

Molecules, 2021, 26 (19), pp.6083. ⟨10.3390/molecules26196083⟩

hal-03096012

Baptiste Villemagne, Arnaud Machelart, Ngoc Chau Tran, Marion Flipo, Martin Moune, Florence Leroux, Catherine Piveteau, Alexandre Wohlkönig, René Wintjens, Xue Li, Ruxandra Gref, Priscille Brodin, Benoit Deprez, Alain Baulard, Nicolas Willand

Fragment-Based Optimized EthR Inhibitors with in Vivo Ethionamide Boosting Activity

ACS Infectious Diseases, 2020, 6 (3), pp.366-378. ⟨10.1021/acsinfecdis.9b00277⟩

hal-03102744

Hugues Prevet, Martin Moune, Abdalkarim Tanina, Christian Kemmer, Adrien Herledan, Rosangela Frita, Alexandre Wohlkönig, Marilyne Bourotte, Baptiste Villemagne, Florence Leroux, Marc Gitzinger, Alain R. Baulard, Benoit Déprez, René Wintjens, Nicolas Willand, Marion Flipo

A fragment-based approach towards the discovery of N-substituted tropinones as inhibitors of Mycobacterium tuberculosis transcriptional regulator EthR2

European Journal of Medicinal Chemistry, 2019, 167, pp.426-438. ⟨10.1016/j.ejmech.2019.02.023⟩

hal-03102772

Nicolas Willand, Marion Flipo, Baptiste Villemagne, Alain Baulard, Benoit Deprez

Recent advances in the design of inhibitors of mycobacterial transcriptional regulators to boost thioamides anti-tubercular activity and circumvent acquired-resistance

Medicinal Chemistry Approaches to Tuberculosis and Trypanosomiasis, pp.131-152, 2019, ⟨10.1016/bs.armc.2019.06.003⟩

hal-03009695

Alexandra Pastor, Arnaud Machelart, Xue Li, Nicolas Willand, Alain Baulard, Priscille Brodin, Ruxandra Gref, Didier Desmaele

A novel codrug made of the combination of ethionamide and its potentiating booster: synthesis, self-assembly into nanoparticles and antimycobacterial evaluation

Organic & Biomolecular Chemistry, 2019, 17 (20), pp.5129 - 5137. ⟨10.1039/c9ob00680j⟩

hal-03177329

Abdalkarim Tanina, Alexandre Wohlkönig, Sameh H. Soror, Marion Flipo, Baptiste Villemagne, Hugues Prevet, Benoit Déprez, Martin Moune, Hélène Perée, Franck Meyer, Alain R. Baulard, Nicolas Willand, René Wintjens

A comprehensive analysis of the protein-ligand interactions in crystal structures of Mycobacterium tuberculosis EthR

Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics, 2018, 1867 (3), pp.248-258. ⟨10.1016/j.bbapap.2018.12.003⟩

hal-01963620

Marion Prieri, Rosangela Frita, Nicolas Probst, Alix Sournia-Saquet, Marilyne Bourotte, Benoit Deprez, Alain R. Baulard, Nicolas Willand

Efficient analoging around ethionamide to explore thioamides bioactivation pathways triggered by boosters in Mycobacterium tuberculosis

European Journal of Medicinal Chemistry, 2018, 159, pp.35-46. ⟨10.1016/j.ejmech.2018.09.038⟩

hal-04463021

Giuseppina Salzano, Jitendra Wankar, Stefano Ottani, Baptiste Villemagne, Alain Baulard, Nicolas Willand, Priscille Brodin, Ilse Manet, Ruxandra Gref

Cyclodextrin-based nanocarriers containing a synergic drug combination: A potential formulation for pulmonary administration of antitubercular drugs

International Journal of Pharmaceutics, 2017, 531 (2), pp.577-587. ⟨10.1016/j.ijpharm.2017.05.030⟩

hal-02263701

Hugues Prevet, Marion Flipo, Pascal Roussel, Benoit Déprez, Nicolas Willand

Microwave-assisted synthesis of functionalized spirohydantoins as 3-D privileged fragments for scouting the chemical space

Tetrahedron Letters, 2016, 57 (26), pp.2888-2894. ⟨10.1016/j.tetlet.2016.05.065⟩

hal-02309782

Baptiste Villemagne, Marion Flipo, Nicolas Blondiaux, Celine Crauste, Sandra Malaquin, Florence Leroux, Catherine Piveteau, Vincent Villeret, Priscille Brodin, Bruno O. Villoutreix, Olivier Sperandio, Sameh H. Soror, Alexandre Wohlkönig, René Wintjens, Benoit Deprez, Alain R. Baulard, Nicolas Willand

Ligand Efficiency Driven Design of New Inhibitors of Mycobacterium tuberculosis Transcriptional Repressor EthR Using Fragment Growing, Merging, and Linking Approaches

Journal of Medicinal Chemistry, 2014, 57 (11), pp.4876-4888. ⟨10.1021/jm500422b⟩

hal-02309788

Céline Crauste, Nicolas Willand, Baptiste Villemagne, Marion Flipo, Eve Willery, Xavier Carette, Martin Moune Dimala, Anne-Sophie Drucbert, Pierre-Marie Danze, Benoit Deprez, Alain R. Baulard

Unconventional surface plasmon resonance signals reveal quantitative inhibition of transcriptional repressor EthR by synthetic ligands

Analytical Biochemistry, 2014, 452, pp.54-66. ⟨10.1016/j.ab.2014.02.011⟩

hal-02309791

Baptiste Villemagne, Céline Crauste, Marion Flipo, Alain R. Baulard, Benoit Déprez, Nicolas Willand

Tuberculosis: The drug development pipeline at a glance

European Journal of Medicinal Chemistry, 2012, 51, pp.1-16. ⟨10.1016/j.ejmech.2012.02.033⟩

pasteur-03525621

Xavier Carette, Nicolas Blondiaux, Eve Willery, Sylviane Hoos, Nathalie Lecat-Guillet, Zoé Lens, Alexandre Wohlkönig, René Wintjens, Sameh H Soror, Frédéric Frénois, Bertrand Dirié, Vincent Villeret, Patrick England, Guy Lippens, Benoit Deprez, Camille Locht, Nicolas Willand, Alain R Baulard

Structural activation of the transcriptional repressor EthR from Mycobacterium tuberculosis by single amino acid change mimicking natural and synthetic ligands

Nucleic Acids Research, 2011, 40 (7), pp.3018 - 3030. ⟨10.1093/nar/gkr1113⟩

inserm-00110437

Patrick Toto, Jean-Claude Gesquiere, Nicolas Cousaert, Benoit Déprez, Nicolas Willand

UFU ('Ullmann-Finkelstein-Ullmann'): a new multicomponent reaction

Tetrahedron Letters, 2006, 47 (28), pp.4973-4978. ⟨10.1016/j.tetlet.2006.04.041⟩

inserm-00110438

Patrick Toto, Jean-Claude Gesquiere, Benoit Déprez, Nicolas Willand

Synthesis of N-(iodophenyl)-amides via an unprecedented Ullmann-Finkelstein tandem reaction

Tetrahedron Letters, 2005, 47, pp.1181-1186. ⟨10.1016/j.tetlet.2005.12.022⟩

inserm-00110439

Nicolas Cousaert, Patrick Toto, Nicolas Willand, Benoit Déprez

Efficient, protection-free Suzuki-Miyaura synthesis of ortho-biphenyltetrazoles

Tetrahedron Letters, 2005, 46, pp.6529-6532. ⟨10.1016/j.tetlet.2005.07.082⟩

inserm-00110444

Nicolas Willand, Terence Beghyn, Guy Nowogrocki, Jean-Claude Gesquiere, Benoit Deprez

Synthesis and structural studies of a novel scaffold for drug discovery: a 4,5-dihydro-3H-spiro[1,5-benzoxazepine-2,4'-piperidine]

Tetrahedron Letters, 2004, 45, pp.1051-1054. ⟨10.1016/j.tetlet.2003.11.079⟩

inserm-00110443

Rebecca Deprez-Poulain, Nicolas Willand, Christophe Boutillon, Guy Nowogrocki, Nathalie Azaroual, Benoit Deprez

A simple reaction to produce small structurally complex and diverse molecules

Tetrahedron Letters, 2004, 45 (27), pp.5287-5290. ⟨10.1016/j.tetlet.2004.05.008⟩

inserm-00110419

Peter Critchley, Nicolas Willand, Atvinder K. Rullay, David H. Crout

Carbohydrate-protein interactions at interfaces: synthesis of thiolactosyl glycolipids and design of a working model for surface plasmon resonance.

Organic & Biomolecular Chemistry, 2003, 1 (6), pp.928-38. ⟨10.1039/b306784j⟩

inserm-00110441

Nicolas Willand, Jurgen Joossens, Jean-Claude Gesquière, André L. Tartar, D. Michael Evans, Michael B. Roe

Solid and solution phase syntheses of the 2-cyanopyrrolidide DPP-IV inhibitor NVP-DPP728

Tetrahedron, 2002, 58, pp.5741-5746. ⟨10.1016/S0040-4020(02)00536-7⟩

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Article dans une revue scientifique