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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.
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
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
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
Fragment-Based Optimized EthR Inhibitors with in Vivo Ethionamide Boosting Activity.
Villemagne B, Machelart A, Tran NC, Flipo M, Moune M, Leroux F, Piveteau C, Wohlkönig A, Wintjens R, Li X, Gref R, Brodin P, Deprez B, Baulard AR, Willand N. Villemagne B, et al. ACS Infect Dis. 2020 Mar 13;6(3):366-378. doi: 10.1021/acsinfecdis.9b00277. Epub 2020 Mar 2. ACS Infect Dis. 2020. PMID: 32011115
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.
On the Hunt for Next-Generation Antimicrobial Agents: An Online Symposium Organized Jointly by the French Society for Medicinal Chemistry (Société de Chimie Thérapeutique) and the French Microbiology Society (Société Française de Microbiologie) on 9-10 December 2021.
Antraygues K, Compagne N, Ruggieri F, Djaout K, Edoo Z, Eveque M, Faïon L, Gioia B, Tangara S, Vieira Da Cruz A, Villemagne B, Flipo M, Baulard A, Willand N. Antraygues K, et al. Among authors: villemagne b. Pharmaceuticals (Basel). 2022 Mar 23;15(4):388. doi: 10.3390/ph15040388. Pharmaceuticals (Basel). 2022. PMID: 35455385 Free PMC article.
40 results