N
Nicolas Willand
Researcher at Pasteur Institute
Publications - 80
Citations - 1525
Nicolas Willand is an academic researcher from Pasteur Institute. The author has contributed to research in topics: Ethionamide & Chemistry. The author has an hindex of 18, co-authored 67 publications receiving 1265 citations. Previous affiliations of Nicolas Willand include French Institute of Health and Medical Research & Lille University of Science and Technology.
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Journal ArticleDOI
Synthetic EthR inhibitors boost antituberculous activity of ethionamide.
Nicolas Willand,Bertrand Dirié,Xavier Carette,Pablo Bifani,Amit Singhal,Matthieu Desroses,Florence Leroux,Eve Willery,Vanessa Mathys,Rebecca Deprez-Poulain,Guy Delcroix,Frédéric Frénois,Frédéric Frénois,Marc Aumercier,Marc Aumercier,Camille Locht,Camille Locht,Vincent Villeret,Vincent Villeret,Benoit Deprez,Alain R. Baulard +20 more
TL;DR: Proof of concept that inhibiting EthR improves the therapeutic index of thiocarbamide derivatives, which should prompt reconsideration of their use as first-line drugs is provided.
Journal ArticleDOI
Tuberculosis: the drug development pipeline at a glance.
Baptiste Villemagne,Céline Crauste,Marion Flipo,Alain R. Baulard,Benoit Deprez,Nicolas Willand +5 more
TL;DR: The pipeline of potential new treatments has been fulfilled with several compounds in clinical trials or preclinical development with promising activities against sensitive and resistant Mycobacterium tuberculosis strains.
Journal ArticleDOI
Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420.
Nicolas Blondiaux,Martin Moune,Matthieu Desroses,Matthieu Desroses,Rosangela Frita,Marion Flipo,Vanessa Mathys,Karine Soetaert,Mehdi Kiass,Vincent Delorme,Vincent Delorme,Kamel Djaout,Vincent Trebosc,Christian Kemmer,René Wintjens,Alexandre Wohlkonig,Rudy Antoine,Ludovic Huot,David Hot,Mireia Coscolla,Mireia Coscolla,Julia Feldmann,Julia Feldmann,Sebastien Gagneux,Sebastien Gagneux,Camille Locht,Priscille Brodin,Marc Gitzinger,Benoit Deprez,Nicolas Willand,Alain R. Baulard +30 more
TL;DR: The first-of-its-kind molecule, named SMARt-420 (Small Molecule Aborting Resistance), not only fully reverses ethionamide-acquired resistance and clears ethion chloride-resistant infection in mice, it also increases the basal sensitivity of bacteria to ethionamide.
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Natural Compounds: Leads or Ideas? Bioinspired Molecules for Drug Discovery
TL;DR: The observations reported here support the design of synthetic compounds inspired from plant alkaloids and their biosynthetic pathway and lead to very efficient syntheses of compounds which complexity matches that of indolomonoterpenic alkaloid.
Journal ArticleDOI
Ethionamide boosters: synthesis, biological activity, and structure-activity relationships of a series of 1,2,4-oxadiazole EthR inhibitors.
Marion Flipo,Matthieu Desroses,Nathalie Lecat-Guillet,Bertrand Dirié,Xavier Carette,Florence Leroux,Catherine Piveteau,Fatma Demirkaya,Zoé Lens,Zoé Lens,Prakash Rucktooa,Prakash Rucktooa,Vincent Villeret,Vincent Villeret,Thierry Christophe,Hee Kyoung Jeon,Camille Locht,Priscille Brodin,Benoit Deprez,Alain R. Baulard,Nicolas Willand +20 more
TL;DR: An extensive structure-activity relationships study with 58 thiophen-2-yl-1,2,4-oxadiazoles as inhibitors of EthR, a transcriptional regulator controling ethionamide bioactivation in Mycobacterium tuberculosis is reported.