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nicolas willand
nicolas willand
Université de Lille
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Tuberculosis: the drug development pipeline at a glance
B Villemagne, C Crauste, M Flipo, AR Baulard, B Déprez, N Willand
European journal of medicinal chemistry 51, 1-16, 2012
2562012
Synthetic EthR inhibitors boost antituberculous activity of ethionamide
N Willand, B Dirie, X Carette, P Bifani, A Singhal, M Desroses, F Leroux, ...
Nature medicine 15 (5), 537-544, 2009
2142009
Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420
N Blondiaux, M Moune, M Desroses, R Frita, M Flipo, V Mathys, ...
Science 355 (6330), 1206-1211, 2017
1392017
Natural compounds: leads or ideas? Bioinspired molecules for drug discovery
T Beghyn, R Deprez‐Poulain, N Willand, B Folleas, B Deprez
Chemical biology & drug design 72 (1), 3-15, 2008
1202008
Ethionamide boosters: synthesis, biological activity, and structure− activity relationships of a series of 1, 2, 4-oxadiazole EthR inhibitors
M Flipo, M Desroses, N Lecat-Guillet, B Dirié, X Carette, F Leroux, ...
Journal of Medicinal Chemistry 54 (8), 2994-3010, 2011
1102011
Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles
J Costa-Gouveia, E Pancani, S Jouny, A Machelart, V Delorme, ...
Scientific reports 7 (1), 5390, 2017
1002017
Ethionamide boosters. 2. Combining bioisosteric replacement and structure-based drug design to solve pharmacokinetic issues in a series of potent 1, 2, 4-oxadiazole EthR inhibitors
M Flipo, M Desroses, N Lecat-Guillet, B Villemagne, N Blondiaux, ...
Journal of medicinal chemistry 55 (1), 68-83, 2012
932012
Exploring Drug Target Flexibility Using in Situ Click Chemistry: Application to a Mycobacterial Transcriptional Regulator
N Willand, M Desroses, P Toto, B Dirie, Z Lens, V Villeret, P Rucktooa, ...
ACS Chemical Biology 5 (11), 1007-1013, 2010
912010
Ligand Efficiency Driven Design of New Inhibitors of Mycobacterium tuberculosis Transcriptional Repressor EthR Using Fragment Growing, Merging, and Linking …
B Villemagne, M Flipo, N Blondiaux, C Crauste, S Malaquin, F Leroux, ...
Journal of medicinal chemistry 57 (11), 4876-4888, 2014
732014
Discovery of Novel N-Phenylphenoxyacetamide Derivatives as EthR Inhibitors and Ethionamide Boosters by Combining High-Throughput Screening and Synthesis
M Flipo, N Willand, N Lecat-Guillet, C Hounsou, M Desroses, F Leroux, ...
Journal of medicinal chemistry 55 (14), 6391-6402, 2012
542012
Intrinsic antibacterial activity of nanoparticles made of β-cyclodextrins potentiates their effect as drug nanocarriers against tuberculosis
A Machelart, G Salzano, X Li, A Demars, AS Debrie, ...
ACS nano 13 (4), 3992-4007, 2019
462019
Structural activation of the transcriptional repressor EthR from Mycobacterium tuberculosis by single amino acid change mimicking natural and synthetic ligands
X Carette, N Blondiaux, E Willery, S Hoos, N Lecat-Guillet, Z Lens, ...
Nucleic acids research 40 (7), 3018-3030, 2012
402012
Synthesis of functionalized 2-isoxazolines as three-dimensional fragments for fragment-based drug discovery
NC Tran, H Dhondt, M Flipo, B Deprez, N Willand
Tetrahedron letters 56 (27), 4119-4123, 2015
382015
Pyridylpiperazine-based allosteric inhibitors of RND-type multidrug efflux pumps
C Plé, HK Tam, A Vieira Da Cruz, N Compagne, JC Jiménez-Castellanos, ...
Nature Communications 13 (1), 115, 2022
352022
Cyclodextrin-based nanocarriers containing a synergic drug combination: A potential formulation for pulmonary administration of antitubercular drugs
G Salzano, J Wankar, S Ottani, B Villemagne, AR Baulard, N Willand, ...
International Journal of Pharmaceutics 531 (2), 577-587, 2017
332017
MALDI imaging techniques dedicated to drug-distribution studies
D Bonnel, R Legouffe, N Willand, A Baulard, G Hamm, B Deprez, ...
Bioanalysis 3 (12), 1399-1406, 2011
332011
A facile and rapid synthesis of N-benzyl-2-substituted piperazines
M Jida, M Soueidan, N Willand, F Agbossou-Niedercorn, L Pelinski, ...
Tetrahedron letters 52 (14), 1705-1708, 2011
332011
Microwave-assisted synthesis of functionalized spirohydantoins as 3-D privileged fragments for scouting the chemical space
H Prevet, M Flipo, P Roussel, B Deprez, N Willand
Tetrahedron Letters 57 (26), 2888-2894, 2016
322016
UFU (‘Ullmann–Finkelstein–Ullmann’): a new multicomponent reaction
P Toto, JC Gesquière, N Cousaert, B Deprez, N Willand
Tetrahedron letters 47 (28), 4973-4978, 2006
312006
New active leads for tuberculosis booster drugs by structure-based drug discovery
NJ Tatum, JW Liebeschuetz, JC Cole, R Frita, A Herledan, AR Baulard, ...
Organic & Biomolecular Chemistry 15 (48), 10245-10255, 2017
292017
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