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Tricyclic SpiroLactams Kill Mycobacteria In Vitro and In Vivo by Inhibiting Type II NADH Dehydrogenases.
Dam S, Tangara S, Hamela C, Hattabi T, Faïon L, Carre P, Antoine R, Herledan A, Leroux F, Piveteau C, Eveque M, Flipo M, Deprez B, Kremer L, Willand N, Villemagne B, Hartkoorn RC. Dam S, et al. Among authors: villemagne b. J Med Chem. 2022 Dec 22;65(24):16651-16664. doi: 10.1021/acs.jmedchem.2c01493. Epub 2022 Dec 6. J Med Chem. 2022. PMID: 36473699 Free PMC article.
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.
Flipo M, Desroses M, Lecat-Guillet N, Villemagne B, Blondiaux N, Leroux F, Piveteau C, Mathys V, Flament MP, Siepmann J, Villeret V, Wohlkönig A, Wintjens R, Soror SH, Christophe T, Jeon HK, Locht C, Brodin P, Déprez B, Baulard AR, Willand N. Flipo M, et al. Among authors: villemagne b. J Med Chem. 2012 Jan 12;55(1):68-83. doi: 10.1021/jm200825u. Epub 2011 Dec 6. J Med Chem. 2012. PMID: 22098589
Tuberculosis: the drug development pipeline at a glance.
Villemagne B, Crauste C, Flipo M, Baulard AR, Déprez B, Willand N. Villemagne B, et al. Eur J Med Chem. 2012 May;51:1-16. doi: 10.1016/j.ejmech.2012.02.033. Epub 2012 Feb 25. Eur J Med Chem. 2012. PMID: 22421275 Review.
Structural and docking studies of potent ethionamide boosters.
Tatum NJ, Villemagne B, Willand N, Deprez B, Liebeschuetz JW, Baulard AR, Pohl E. Tatum NJ, et al. Among authors: villemagne b. Acta Crystallogr C. 2013 Nov;69(Pt 11):1243-50. doi: 10.1107/S0108270113028126. Epub 2013 Oct 24. Acta Crystallogr C. 2013. PMID: 24192167
Ligand efficiency driven design of new inhibitors of Mycobacterium tuberculosis transcriptional repressor EthR using fragment growing, merging, and linking approaches.
Villemagne B, Flipo M, Blondiaux N, Crauste C, Malaquin S, Leroux F, Piveteau C, Villeret V, Brodin P, Villoutreix BO, Sperandio O, Soror SH, Wohlkönig A, Wintjens R, Deprez B, Baulard AR, Willand N. Villemagne B, et al. J Med Chem. 2014 Jun 12;57(11):4876-88. doi: 10.1021/jm500422b. Epub 2014 May 28. J Med Chem. 2014. PMID: 24818704
A comprehensive analysis of the protein-ligand interactions in crystal structures of Mycobacterium tuberculosis EthR.
Tanina A, Wohlkönig A, Soror SH, Flipo M, Villemagne B, Prevet H, Déprez B, Moune M, Perée H, Meyer F, Baulard AR, Willand N, Wintjens R. Tanina A, et al. Among authors: villemagne b. Biochim Biophys Acta Proteins Proteom. 2019 Mar;1867(3):248-258. doi: 10.1016/j.bbapap.2018.12.003. Epub 2018 Dec 13. Biochim Biophys Acta Proteins Proteom. 2019. PMID: 30553830 Free article.
A fragment-based approach towards the discovery of N-substituted tropinones as inhibitors of Mycobacterium tuberculosis transcriptional regulator EthR2.
Prevet H, Moune M, Tanina A, Kemmer C, Herledan A, Frita R, Wohlkönig A, Bourotte M, Villemagne B, Leroux F, Gitzinger M, Baulard AR, Déprez B, Wintjens R, Willand N, Flipo M. Prevet H, et al. Among authors: villemagne b. Eur J Med Chem. 2019 Apr 1;167:426-438. doi: 10.1016/j.ejmech.2019.02.023. Epub 2019 Feb 10. Eur J Med Chem. 2019. PMID: 30784877
Intrinsic Antibacterial Activity of Nanoparticles Made of β-Cyclodextrins Potentiates Their Effect as Drug Nanocarriers against Tuberculosis.
Machelart A, Salzano G, Li X, Demars A, Debrie AS, Menendez-Miranda M, Pancani E, Jouny S, Hoffmann E, Deboosere N, Belhaouane I, Rouanet C, Simar S, Talahari S, Giannini V, Villemagne B, Flipo M, Brosch R, Nesslany F, Deprez B, Muraille E, Locht C, Baulard AR, Willand N, Majlessi L, Gref R, Brodin P. Machelart A, et al. Among authors: villemagne b. ACS Nano. 2019 Apr 23;13(4):3992-4007. doi: 10.1021/acsnano.8b07902. Epub 2019 Mar 8. ACS Nano. 2019. PMID: 30822386 Free PMC article.
40 results