Recherche - Archive ouverte HAL Accéder directement au contenu

Filtrer vos résultats

29 résultats
Page :
triés par
Image document

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

 Benoit Deprez , Damien Bosc , Julie Charton , Cyril Couturier , Rebecca Deprez-Poulain , et al.
Molecules, 2021, 26 (19), pp.6083. ⟨10.3390/molecules26196083⟩
Article dans une revue hal-04465890v1
Image document

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

 Baptiste Villemagne , Marion Flipo , Nicolas Blondiaux , Celine Crauste , Sandra Malaquin , et al.
Journal of Medicinal Chemistry, 2014, 57 (11), pp.4876-4888. ⟨10.1021/jm500422b⟩
Article dans une revue hal-02309782v1
Image document

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

 Abdalkarim Tanina , Alexandre Wohlkönig , Sameh H. Soror , Marion Flipo , Baptiste Villemagne , et al.
Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics, 2018, 1867 (3), pp.248-258. ⟨10.1016/j.bbapap.2018.12.003⟩
Article dans une revue hal-03177329v1
Image document

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

 Peter Critchley , Nicolas Willand , Atvinder K. Rullay , David H. Crout
Organic & Biomolecular Chemistry, 2003, 1 (6), pp.928-38. ⟨10.1039/b306784j⟩
Article dans une revue inserm-00110419v1
Image document

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

 Patrick Toto , Jean-Claude Gesquiere , Benoit Déprez , Nicolas Willand
Tetrahedron Letters, 2005, 47, pp.1181-1186. ⟨10.1016/j.tetlet.2005.12.022⟩
Article dans une revue inserm-00110438v1
Image document

Tuberculosis: The drug development pipeline at a glance

 Baptiste Villemagne , Céline Crauste , Marion Flipo , Alain R. Baulard , Benoit Déprez , et al.
European Journal of Medicinal Chemistry, 2012, 51, pp.1-16. ⟨10.1016/j.ejmech.2012.02.033⟩
Article dans une revue hal-02309791v1

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

 Marion Prieri , Rosangela Frita , Nicolas Probst , Alix Sournia-Saquet , Marilyne Bourotte , et al.
European Journal of Medicinal Chemistry, 2018, 159, pp.35-46. ⟨10.1016/j.ejmech.2018.09.038⟩
Article dans une revue hal-01963620v1
Image document

Discovery of the first Mycobacterium tuberculosis MabA (FabG1) inhibitors through a fragment-based screening

 Léo Faion , Kamel Djaout , Rosangela Frita , Catalin Pintiala , Francois-Xavier Cantrelle , et al.
European Journal of Medicinal Chemistry, 2020, 200, pp.112440. ⟨10.1016/j.ejmech.2020.112440⟩
Article dans une revue hal-02988077v1
Image document

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

 Nicolas Willand , Jurgen Joossens , Jean-Claude Gesquière , André L. Tartar , D. Michael Evans , et al.
Tetrahedron, 2002, 58, pp.5741-5746. ⟨10.1016/S0040-4020(02)00536-7⟩
Article dans une revue inserm-00110441v1
Image document

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

 Benjamin Guieu , Jean-Pierre Jourdan , Aurore Dreneau , Nicolas Willand , Christophe Rochais , et al.
Drug Discovery Today, 2021, 26 (2), pp.315-328. ⟨10.1016/j.drudis.2020.11.026⟩
Article dans une revue hal-03969988v1
Image document

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

 Céline Crauste , Nicolas Willand , Baptiste Villemagne , Marion Flipo , Eve Willery , et al.
Analytical Biochemistry, 2014, 452, pp.54-66. ⟨10.1016/j.ab.2014.02.011⟩
Article dans une revue hal-02309788v1
Image document

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

 Hugues Prevet , Martin Moune , Abdalkarim Tanina , Christian Kemmer , Adrien Herledan , et al.
European Journal of Medicinal Chemistry, 2019, 167, pp.426-438. ⟨10.1016/j.ejmech.2019.02.023⟩
Article dans une revue hal-03102744v1
Image document

Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles

 Joana Costa-Gouveia , Elisabetta Pancani , Samuel J Jouny , Arnaud Machelart , Vincent Delorme , et al.
Scientific Reports, 2017, 7 (1), ⟨10.1038/s41598-017-05453-3⟩
Article dans une revue hal-02367442v1
Image document

A simple reaction to produce small structurally complex and diverse molecules

 Rebecca Deprez-Poulain , Nicolas Willand , Christophe Boutillon , Guy Nowogrocki , Nathalie Azaroual , et al.
Tetrahedron Letters, 2004, 45 (27), pp.5287-5290. ⟨10.1016/j.tetlet.2004.05.008⟩
Article dans une revue inserm-00110443v1

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

 Hugues Prevet , Marion Flipo , Pascal Roussel , Benoit Déprez , Nicolas Willand
Tetrahedron Letters, 2016, 57 (26), pp.2888-2894. ⟨10.1016/j.tetlet.2016.05.065⟩
Article dans une revue hal-02263701v1
Image document

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

 Nicolas Cousaert , Patrick Toto , Nicolas Willand , Benoit Déprez
Tetrahedron Letters, 2005, 46, pp.6529-6532. ⟨10.1016/j.tetlet.2005.07.082⟩
Article dans une revue inserm-00110439v1
Image document

Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420

 Nicolas Blondiaux , Martin Moune , Matthieu Desroses , Rosangela Frita , Marion Flipo , et al.
Science, 2017, 355 (6330), pp.1206-1211. ⟨10.1126/science.aag1006⟩
Article dans une revue hal-03102877v1
Image document

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

 Xavier Carette , Nicolas Blondiaux , Eve Willery , Sylviane Hoos , Nathalie Lecat-Guillet , et al.
Nucleic Acids Research, 2011, 40 (7), pp.3018 - 3030. ⟨10.1093/nar/gkr1113⟩
Article dans une revue pasteur-03525621v1
Image document

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

 Nicolas Willand , Marion Flipo , Baptiste Villemagne , Alain Baulard , Benoit Deprez
Medicinal Chemistry Approaches to Tuberculosis and Trypanosomiasis, pp.131-152, 2019, ⟨10.1016/bs.armc.2019.06.003⟩
Chapitre d'ouvrage hal-03102772v1
Image document

Intrinsic Antibacterial Activity of Nanoparticles Made of β-Cyclodextrins Potentiates Their Effect as Drug Nanocarriers against Tuberculosis

 Arnaud Machelart , Giuseppina Salzano , Xue Li , Aurore Demars , Anne-Sophie Debrie , et al.
ACS Nano, 2019, 13 (4), pp.3992-4007. ⟨10.1021/acsnano.8b07902⟩
Article dans une revue hal-02367420v1
Image document

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

 Alexandra Pastor , Arnaud Machelart , Xue Li , Nicolas Willand , Alain Baulard , et al.
Organic & Biomolecular Chemistry, 2019, 17 (20), pp.5129 - 5137. ⟨10.1039/c9ob00680j⟩
Article dans une revue hal-03009695v1

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

 Giuseppina Salzano , Jitendra Wankar , Stefano Ottani , Baptiste Villemagne , Alain Baulard , et al.
International Journal of Pharmaceutics, 2017, 531 (2), pp.577-587. ⟨10.1016/j.ijpharm.2017.05.030⟩
Article dans une revue hal-04463021v1
Image document

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

 Francesca Ruggieri , Nina Compagne , Kevin Antraygues , Maxime Eveque , Marion Flipo , et al.
European Journal of Medicinal Chemistry, 2023, 256, pp.115413. ⟨10.1016/j.ejmech.2023.115413⟩
Article dans une revue hal-04093378v1
Image document

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

 Patrick Toto , Jean-Claude Gesquiere , Nicolas Cousaert , Benoit Déprez , Nicolas Willand
Tetrahedron Letters, 2006, 47 (28), pp.4973-4978. ⟨10.1016/j.tetlet.2006.04.041⟩
Article dans une revue inserm-00110437v1
Image document

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

 Nicolas Willand , Terence Beghyn , Guy Nowogrocki , Jean-Claude Gesquiere , Benoit Deprez
Tetrahedron Letters, 2004, 45, pp.1051-1054. ⟨10.1016/j.tetlet.2003.11.079⟩
Article dans une revue inserm-00110444v1
Image document

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

 Kevin Antraygues , Mathieu Maingot , Birgit Schellhorn , Vincent Trebosc , Marc Gitzinger , et al.
European Journal of Medicinal Chemistry, 2022, 238, pp.114515. ⟨10.1016/j.ejmech.2022.114515⟩
Article dans une revue hal-04017312v1

The small-molecule SMARt751 reverses Mycobacterium tuberculosis resistance to ethionamide in acute and chronic mouse models of tuberculosis

 Marion Flipo , Rosangela Frita , Marilyne Bourotte , María Martínez-Martínez , Markus Boesche , et al.
Science Translational Medicine, 2022, 14 (643), ⟨10.1126/scitranslmed.aaz6280⟩
Article dans une revue hal-04465505v1
Image document

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

 Léo Faïon , Kamel Djaout , Catalin Pintiala , Catherine Piveteau , Florence Leroux , et al.
Pharmaceuticals, 2023, 16 (3), pp.335. ⟨10.3390/ph16030335⟩
Article dans une revue hal-04007450v1
Image document

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

 Baptiste Villemagne , Arnaud Machelart , Ngoc Chau Tran , Marion Flipo , Martin Moune , et al.
ACS Infectious Diseases, 2020, 6 (3), pp.366-378. ⟨10.1021/acsinfecdis.9b00277⟩
Article dans une revue hal-03096012v1
Page :