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Page 1
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. Among authors: brodin p. 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
Ethionamide boosters: synthesis, biological activity, and structure-activity relationships of a series of 1,2,4-oxadiazole EthR inhibitors.
Flipo M, Desroses M, Lecat-Guillet N, Dirié B, Carette X, Leroux F, Piveteau C, Demirkaya F, Lens Z, Rucktooa P, Villeret V, Christophe T, Jeon HK, Locht C, Brodin P, Déprez B, Baulard AR, Willand N. Flipo M, et al. Among authors: brodin p. J Med Chem. 2011 Apr 28;54(8):2994-3010. doi: 10.1021/jm200076a. Epub 2011 Apr 1. J Med Chem. 2011. PMID: 21417236
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: brodin p. J Med Chem. 2012 Jan 12;55(1):68-83. doi: 10.1021/jm200825u. Epub 2011 Dec 6. J Med Chem. 2012. PMID: 22098589
Discovery of novel N-phenylphenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining high-throughput screening and synthesis.
Flipo M, Willand N, Lecat-Guillet N, Hounsou C, Desroses M, Leroux F, Lens Z, Villeret V, Wohlkönig A, Wintjens R, Christophe T, Kyoung Jeon H, Locht C, Brodin P, Baulard AR, Déprez B. Flipo M, et al. Among authors: brodin p. J Med Chem. 2012 Jul 26;55(14):6391-402. doi: 10.1021/jm300377g. Epub 2012 Jul 17. J Med Chem. 2012. PMID: 22738293
Discovery of Q203, a potent clinical candidate for the treatment of tuberculosis.
Pethe K, Bifani P, Jang J, Kang S, Park S, Ahn S, Jiricek J, Jung J, Jeon HK, Cechetto J, Christophe T, Lee H, Kempf M, Jackson M, Lenaerts AJ, Pham H, Jones V, Seo MJ, Kim YM, Seo M, Seo JJ, Park D, Ko Y, Choi I, Kim R, Kim SY, Lim S, Yim SA, Nam J, Kang H, Kwon H, Oh CT, Cho Y, Jang Y, Kim J, Chua A, Tan BH, Nanjundappa MB, Rao SP, Barnes WS, Wintjens R, Walker JR, Alonso S, Lee S, Kim J, Oh S, Oh T, Nehrbass U, Han SJ, No Z, Lee J, Brodin P, Cho SN, Nam K, Kim J. Pethe K, et al. Among authors: brodin p. Nat Med. 2013 Sep;19(9):1157-60. doi: 10.1038/nm.3262. Epub 2013 Aug 4. Nat Med. 2013. PMID: 23913123 Free article.
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. Among authors: brodin p. J Med Chem. 2014 Jun 12;57(11):4876-88. doi: 10.1021/jm500422b. Epub 2014 May 28. J Med Chem. 2014. PMID: 24818704
2-Carboxyquinoxalines kill mycobacterium tuberculosis through noncovalent inhibition of DprE1.
Neres J, Hartkoorn RC, Chiarelli LR, Gadupudi R, Pasca MR, Mori G, Venturelli A, Savina S, Makarov V, Kolly GS, Molteni E, Binda C, Dhar N, Ferrari S, Brodin P, Delorme V, Landry V, de Jesus Lopes Ribeiro AL, Farina D, Saxena P, Pojer F, Carta A, Luciani R, Porta A, Zanoni G, De Rossi E, Costi MP, Riccardi G, Cole ST. Neres J, et al. Among authors: brodin p. ACS Chem Biol. 2015 Mar 20;10(3):705-14. doi: 10.1021/cb5007163. Epub 2014 Dec 9. ACS Chem Biol. 2015. PMID: 25427196
374 results